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Comprehensive review on additives of topical dosage forms for drug delivery
Abstract
Abstract Skin is the largest organ of the human body and plays the most important role in protecting against pathogen and foreign matter. Three important modes such as topical, regional and transdermal are widely used for delivery of various dosage forms. Among these modes, the topical dosage forms are preferred because it provides local therapeutic activity when applied to the skin or mucous membranes. Additives or pharmaceutical excipients (non-drug component of dosage form) are used as inactive ingredients in dosage form or tools for structuring dosage forms. The main use of topical dosage form additives are controling the extent of absorption, maintaining the viscosity, improving the stability as well as organoleptic property and increasing the bulk of the formulation. The overall goal of this article is to provide the clinician with information related to the topical dosage form additives and their current major applications against various diseases.
... TDS patches, sometimes known as transdermal patches, are devices that are applied on the skin and vary in composition and manufacture method. As a result, they use various techniques to release their active components 5,7,8,18 . ...
... Glycerin, Hydroxyethyl urea, betaine, sodium PCA, Sodium-L-Lactate, and other humectants are examples. [5] Perfumes: It's used in a number of items to add a pleasant scent and disguise the odour of some substances. It's found in all kinds of cosmetics. ...
... 4. It is non-intrusive in nature. 5. It results in high patient satisfaction. ...
Creams are a type of pharmaceutical product used for daily skin care, as well as medicated and non-medicated applications. It is also regarded as a vital component of cosmetics. When the dosage form is creams, the route of delivery is the skin. The rate of medication absorption and penetration is influenced by a variety of factors in the skin. The topical medication delivery system is a method of delivering drugs to the skin. Topical medication administration has the advantage of bypassing first-pass metabolism, hydrating the skin, and providing emollient qualities. Creams are viscous or semisolid emulsions that come in O/W or W/O dosage forms and have a viscosity that changes depending on the quantities of oil and water in them. In terms of functions and qualities, there is a vast range of creams available. Pharmaceutical creams are used for a range of purposes, including cleansing, beautifying, hydrating, and protecting against bacteria and fungi, as well as treating skin wounds. Water, fats, waxes, emollients, colors, scents, and other common ingredients are employed in the creation of practically every cream, resulting in a standard formulation. There are various evaluation parameters available for creams which help the product to match its standard quality eg. pH, viscosity, stability, spreadability, etc.
... Numerous considerations influence the selection of bases for semisolid dosage forms. The distribution environment, the end product's shelf life, the type of active ingredient at the site of action, and the desired therapeutic effect [3,22] . The base should not cause irritation, sensitization and in order to be compatible with the skin and the active substances to be incorporated, it must be smooth, inert, odorless, physically stable, and chemically inert. ...
... Conventional topical formulations such as (creams, ointments, pastes, gels, and others) have various disadvantages, including adhering to the skin, causing patient discomfort during application, being less spreadable and requiring rubbing application, and rapidly evaporating from the skin. To avoid these limitations, emulgel formulation was developed [22] . ...
In recent years, gels have been preferentially used for cosmetics and topical pharmaceutical preparations due to their favorable characteristics, such as being greaseless, readily spreadable and easily removable. However, one obstacle that faced it was the inability to enclose hydrophobic compounds. Therefore, a novel approach was developed to circumvent this limitation by mixing the gel with an emulsion, which led to creation of a new topical drug delivery system known as emulgel. Emulgel preserves all favorable features of gel and provides also dual release for drug, thus can be utilized effectively in controlling release and absorption of medication after topical application. Emulgel preparation requires coherent steps, this includes preparation of emulsion and gel and determining their mixing ratio. Finally, the prepared emulgels should be evaluated to ensure their suitability and efficacy for the topical application.
... Advantages [22] Advantages and Disadvantages of cream as a topical drug delivery system. It is the easiest way to deliver a drug. ...
... Disadvantages [22] Skin irritation Some drugs show low penetrable through the skin. Possibility of allergic reactions. ...
Creams are considered an important part of cosmetic product as topical preparations from cosmetic purposes, pharmaceutical creams having a various variety of applications for ex. Beautifying, moisturizing, cleansing etc. for skin protection against bacterial and fungal infections. Creams are for the most part solid or liquid emulsions. If they set solid, they are emulsified in molten state by heating the ingredients to liquify them and permitting them to solidify after being filled into the packages. As already indicated, these emulsions either oil in water or water in oil types. The former type of emulsion predominates in the cream field. The introduction of numerous new emulsification aids and cream bases has made possible in recent years a greater variety of creams than was formerly possible. By numerous combinations of these newer products with the old bees' wax-mineral oil-borax-water cream type innumerable cream formulae may be devised. Creams have the number of advantages like easy to apply, more effective compares to other avoid risk. The functions of skin creams are to protect the skin against harshness from the environment and any dry conditions of the skin.
... A load of 400 g (consisting of a beaker filled with water and an inverted petri dish lid) was placed exactly on the cream. The study was conducted for different time intervals, i.e., (30,60,90, 120 and 150) s. The spreadability was calculated according to the following equation. ...
... The formulation FC-C-D also shows an antifungal activity of 3.2 cm which is slightly lower than that of FC-C-C. The higher antifungal activity of FC-C-C and FC-C-D compared to FC-C-A and FC-C-B is due to the presence of borax [30], which is active against C. albicans. The results obtained also confirmed that the antifungal activity increases with the increase of stearic acid. ...
The aim of the present study was to formulate a fluconazole cream for the treatment of Candida albicans. The optimized cream formulation was prepared using stearic acid, oleic acid, beeswax and borax. The uniform distribution of the active ingredient fluconazole could be confirmed in all formulated creams. The FC-C-C formulation showed satisfactory spreadability and extrudability. FC-C-C delivered (95.07 ± 15.85)% in only 36 h, and the formulation released the drug by an anomalous diffusion mechanism. The viscosity of FC-C-C was found to be (63.20 ± 0.83) cP. The antifungal study and animal studies confirmed that the prepared formulation is non-irritant and has an enhanced antifungal activity that reduces the side effects of fluconazole. The studies confirm that the prepared formulation may be useful for the treatment of Candida albicans.
... The skin contributes to around 10% of the net body mass and is mainly composed of three to four layers. The order of the layers is arranged from the peripheral to the profound layers as follows: stratum corneum (SC), viable epidermis and dermis [8,9]. Figure (1.1) schematically illustrates a cross section through human skin layers. ...
... ; VrN=p(6); kve=p(5); kd=p(4); td=p(1); fun = @(s) 1/s/((1/(ClrN+VrN*s*td)+1/kve+1/kd+1/(VdN*s*td))*cosh(sqrt((s)*td))... +(1/sqrt((s)*td)+sqrt((s)*td)*(1/kd+1/(VdN*s*td))*(1/kve+1/(ClrN+VrN*s*td)))... *sinh(sqrt((s)*td))); Jsx=@(s) fun(s); (3)); dose=p (2) (3) 233 j(i)=(n+1)*f(Uk(i,n))*(Uk(i,n)-Uk(i,n+3)/Kr)/(1+(n+1)*f(Uk(i,n))/kve);% w(i)=Uk(i,n+2); end FC=j; ZC=w; end function dy = compartmentDC(y,n,p) td=p(1); VdN=p(3); kd=p(4); kve=p(5); VrN=p(6); ClrN=p(7); Kr=p(8); beta=p(9); f=@(u) exp(beta*u); dy = zeros(n+3,1); dy(n+2)=(n+1)*(f(y(n+2))/(1+(n+1)*f(y(n+2))/kd))*(y(1)-y(n+2))/(VdN*td); % dCv/dt dy(1)=n*(n+1)*(f(y(n+2))/(1+(n+1)*f(y(n+2))/kd)*(y(n+2)-y(1))+(y(2)y(1))*f(y(1)))/td; for i = 2:n-1 dy(i)=n*(n+1)*((y(i-1)-y(i))*f(y(i-1))+(y(i+1)-y(i))*f(y(i)))/td; end dy(n) = n*(n+1)*((y(n-1)-y(n))*f(y(n-1))+f(y(n))/(1+(n+1)*f(y(n))/kve)*(y(n+3)/Kry(n)))/td; dy(n+1)=y(n)*(n+1)*f(y(n))/(1+(n+1)*f(y(n))/kve);% AD/h |(n+1) kp Cn(t) dt = Q dy(n+3)=((n+1)*(f(y(n))/(1+(n+1)*f(y(n))/kve))*(Kr*y(n)-y(n+3))-ClrN*y(n+3))/(VrN*td); (7); Kr=p(8); beta=p (9); f=@(c) exp(beta*c); df=@(c) beta.*exp(beta*c); n=Nfinite; a=(Nfinite-1)^2/td; dy = zeros(n+3,1); dy(n+2)=kd*(y(1)-y(n+2))/(VdN*td); % dCv/dt dy(1)=2*a*f(y(1))*(y(2)-y(1)-(y(1)-y(n+2))*kd/(Nfinite-1)/f(y(1)))... +((y(1)-y(n+2))*kd/f(y(1))).^2*df(y(1))/td; for i = 2:Nfinite-1 dy(i)=a*f(y(i))*(y(i-1)-2*y(i)+y(i+1))+0.25*((Nfinite-1)*(y(i+1)-y(i-1))).^2.*df(y(i))./td; ...
In this thesis, we have developed a novel mathematical model using a compartmental
approach. The proposed model enables for simulating solute transport across the stratum corneum (SC) in a variety of exposure scenarios in percutaneous drug delivery systems.
The obtained results were compared with the diffusion model outcomes – which can be
considered the current ‘golden standard’ for modelling skin transport – and showed a
good agreement. The mathematical foundations of the model are relatively simple and
better aligned with the physiology of the stratum corneum. In addition, this work shows
that performing a numerical simulation using the compartmental model is less demanding
than using the diffusing model, especially for complex exposure scenarios, and can be
performed using free software, such as Python.
The research findings of this thesis contribute towards a better understanding of transport
phenomena across the skin. Also, the compartmental model proposed in this work can be
used to describe transport phenomena in the membrane. Due to the similarity between the
governing equations of diffusion and heat transfer, the proposed approach also offers a
mathematical framework for studying heat transfer problems in biomaterials with
minimum model development or computational efforts.
... Glycerine, hydroxyethyl urea, betaine, sodium-L-lactate, and other humectants are some examples. Humectants are also used in shampoo to help hydrate hair and counter the drying effect of surfactants [7]. They also help with low temperature stabilization and freeze / thaw, acting as antifreeze and maintaining shampoo clarity at low temperatures. ...
... Vitamins are necessary for the proper functioning of the physiological functions of the body and the skin. Vitamins A, B, C, E and others are commonly used in the formulation of the cream [7]. Skincare products contain preservatives to help stop microbe contamination and instability during formulation, shipping, storage, and consumer use. ...
... The diameter of the zone of inhibition for negative control (mm) S. aureus 30 ...
... Herbal soaps in 50 g in weight were formed by adding plant extracts, distilled water, stearic acid and natural volatile oil into the glycerin soap base. However, the active ingredients and added excipients should be compatible with the vehicle 30 . ...
... It is essential to explore new natural active compounds and semi-solid formulations that ensure formulation efficacy and are suitable for daily skin care and alleviating symptoms of inflammatory diseases. For the treatment of skin conditions, semi-solid pharmaceutical preparations such as ointments, creams, gels, and emulgels are commonly used [19,20]. A crucial aspect is selecting an appropriate base for the formulation. ...
Balsam poplar buds have been used for wound healing and treating irritated skin in traditional medicine. Balsam poplar buds extracts exhibit anti-inflammatory, antioxidant, and antimicrobial effects. In recent years, scientific research has begun to validate some of these traditional uses, leading to an increased interest in balsam poplar buds as a potential source of natural remedies in modern medicine. The study aims to simulate semi-solid pharmaceutical forms with balsam poplar buds extract and evaluate their quality through biopharmaceutical research. The active compounds identified in Lithuanian poplar buds were p-coumaric acid, cinnamic acid, caffeic acid, galangin, pinocembrin, pinobanksin, and salicin. In gels, pH values ranged from 5.85 ± 0.05 to 5.95 ± 0.07. The determined pH values of emulgels ranged from 5.13 ± 0.05 to 5.66 ± 0.15. After 6 h, the release of active compounds from gels and emulgels ranged from 47.40 ± 2.41% to 71.17 ± 3.54. p-coumaric acid dominates in the balsam poplar buds extracts. The pH values of the prepared sem-solid pharmaceutical forms are suitable for use on the skin. The viscosity of the formulations depends on the amount of gelling agent. All formulations showed antioxidant activity. It is relevant to conduct a more extensive study on the influence of the chosen carrier on the release of active compounds from semi-solid formulations with an extract of balsam poplar buds.
... There are a variety of potential sites for transdermal absorption on the skin due to its enormous surface area and convenience of access [1][2][3][4][5][6]. Ointments, creams, large adhesive patches, plasters, poultices, and cataplasms are all classic topical formulations [7]. Simple, low-dose molecules and active chemicals are what really make up first-generation TDDS, which are released locally or topically. ...
... Nevertheless, recent studies have revealed that capsaicin formulations containing ≥ 1.0% capsaicin such as capsaicin patch (8.0%) may prolong duration of drug action, reduce dosing frequency and improve patient adherence [13]. Aqueous creams are particularly attractive to patients for topical application because they are less greasy and readily washed off skin and clothes [21]. In order to enhance drug permeation with aqueous formulations, permeation enhancers such as propylene glycol are incorporated into topical creams [22]. ...
Purpose: Conventional topical capsaicin creams are often unavailable and unaffordable to the larger patient populations in developing countries. There is a need to formulate cost-effective alternatives using locally available polymers as cream base. This study aimed to formulate oil-in-water Grewia mollis mucilage-hydroxypropyl methylcellulose (GMM-HPMC) based capsaicin creams from locally available capsicum fruits and evaluation of their quality attributes.
Methods: Capsaicin was quantified from acetone extracts of Capsicum fruits (C. frutescens, C. pubescens and C. chinense) using high performance liquid chromatography (HPLC). Extract of C. chinense which had higher capsaicin content was used to formulate six different cream types with varied concentrations of GMM and/or HPMC as polymeric base. The creams were assessed for their organoleptic properties, pH, specific gravity, conductivity, viscosity, spreadability, oil globule size, microbial load and stability profiles using standard methods and protocols.
Results: The FTIR spectroscopic analysis confirmed the presence of capsaicin in all the Capsicum fruit extracts; HPLC quantification of each of the fruit extracts indicated the presence of both capsaicin; C. chinense: (36153 ppm) > C. frutescens: (7860 ppm) > C. pubescens: (4549 ppm) and dihydrocapsaicin; C. chinense (11044 ppm) > C. frutescens (6920 ppm) > C. pubescens (2828 ppm) as constituents. Formulated o/w creams were light to deep brick red in colour, with pH (6.11-6.44); specific gravity (1.00-1.03); electrical conductivity (292-1958 μS/cm); viscosity (2810-9190 mPas); spreadability (4.0-5.5 cm) and globule size (13 ± 8 μm to 91 ± 20 μm). The creams had satisfactory microbial load profiles and remained stable at 25 ± 2 °C but had varying degrees of stability at 40 ± 2 °C storage temperatures.
The optimized formulations of the creams (FB, FE and FF) contained GMM as the mono polymeric base system, while GMM10:HPMC10 and GMM15:HPMC10 were the co-polymeric base systems, respectively.
Conclusion: This study has shown the suitability of Grewia mollis mucilage singly used or in combination with hydroxypropyl methylcellulose as co-polymeric cream base. Formulated creams had desirable physicochemical properties and they may find better patient acceptance when compared with imported brands as a result of their potential low cost.
... It is observed that crude drugs used as poultice is a common practice among the tribal as also reported by Roosita et al.(2008) and Upadhyay et al. (2010). Various active drug molecules of topical dosage forms were quite effectively absorbed through the biological membrane and work onto the target site of the affected tissue (Garg et al. 2014). That is why the topical administration process of herbal drugs is preferred for treatment of different ailments of muscular and skin related disorders which were in accordance with folk-claims documented in some ethnobotanical studies (Wirth et al. 2005, Ayyanar & Ignacimuthu 2011, Rahaman & Karmakar 2015, Shedoeva et al. 2019. ...
A Quantitative ethnobotanical approach to assess knowledge richness on the use of plants among the Santal Medicine Men of Birbhum district, West Bengal, India
... It is observed that crude drugs used as poultice is a common practice among the tribal as also reported by Roosita et al.(2008) and Upadhyay et al. (2010). Various active drug molecules of topical dosage forms were quite effectively absorbed through the biological membrane and work onto the target site of the affected tissue (Garg et al. 2014). That is why the topical administration process of herbal drugs is preferred for treatment of different ailments of muscular and skin related disorders which were in accordance with folk-claims documented in some ethnobotanical studies (Wirth et al. 2005, Ayyanar & Ignacimuthu 2011, Rahaman & Karmakar 2015, Shedoeva et al. 2019. ...
... Balsam termasuk sediaan salep yang mudah dioleskan bentuk sediaan balsam dapat meningkatkan hidrasi dan suhu kulit, meningkatkan penyerapan obat ke kulit, oklusif, dan kebanyakan sediaan balsam tidak mengandung tambahan pengawet sehingga dapat menurunkan resiko alergi (Garg et al., 2015). Basis utama balsam adalah Paraffin, vaselin album atau flavum, campora, menthol, dan lilin atau cera alba (Warditiani et al., 2020). ...
Balsam merupakan salah satu bentuk sediaan setengah padat yang digunakan sebagai obat luar. Balsam tersebut memiliki indikasi untuk meredakan nyeri pada sendi dengan memberikan sensasi hangat, balsam digunakan sebagai aromaterapi, pada sediaan balsam kali ini, digunakan cera alba sebagai zat penstabil (stabilizing agent). Penelitian ini bertujuan untuk membuat sediaan balsam sesuai dengan formula, menentukan konsistensi sediaan balsam, meliputi uji pH, organoleptis, homogenitas, daya lekat dan daya sebar sediaan balsam. Hasil evaluasi menunjukkan bahwa balsam dengan menggunakan basis cera alba sebesar 15% memiliki pH yang cocok untuk kulit, daya sebar yang sesuai, daya lekat yang baik, dan organoleptis yang memenuhi syarat SNI. Sediaan balsam aromaterapi memiliki homogenitas yang baik, serta tidak mengalami perubahan warna dan bau setelah 14 hari. Berdasarkan penelitian yang telah dilakukan, dapat disimpulkan bahwa minyak lemon (oleum citri) dapat diformulasikan menjadi sediaan balsam aromaterapi yang stabil dan memenuhi syarat serta dapat bertahan selama 14 hari dengan konsentrasi cera alba sebesar 15%.
... However, the possibility to apply salicylic acid and obtain the related medicinal preparations is limited because high concentrations of the acid produce undesirable side effects: a detrimental effect on the gastrointestinal mucosa, disturbance of the kidney functions, and others [21,22]. At present, 1-2% alcoholic solutions of salicylic acid and ointments with the salicylic acid content from 2 to 10% are used in the national medical practice for outward application [23][24][25]. ...
For the first time an advanced carbon sorbent modified with salicylic acid for medicinal and veterinary applications was synthesized by the adsorption from solutions. Optimal parameters of the modification were determined: Solvent, “carbon sorbent–modifier” ratio, concentration of salicylic acid, equilibration time of the process in the “sorbent–salicylic acid solution” system, pH, and process temperature. The effect of the drying parameters on stability and amount of oxygen-containing groups on the carbon sorbent surface after modification was established. Physicochemical properties of the carbon sorbent and sorbents modified with different concentrations of salicylic acid were investigated: textural characteristics, qualitative and quantitative compositions of the surface functional groups, and amount of the deposited modifier. The possibility of salicylic acid desorption into the media simulating biological fluids, particularly the gastrointestinal medium, was explored. Adsorption characteristics of the carbon sorbent and sorbents modified with different concentrations of salicylic acid with respect to organic dyes—methylene blue and metanil yellow in a wide range of operating concentrations—were revealed.
Graphical abstract
... Skin quality and beauty have become significant concerns of the worldwide population, and they consequently drive ongoing research and innovation in the field to develop more effective formulations for the penetration and permeation of the skin by pharmaceutical or cosmetic ingredients (API/ACI). Commercial cosmetics or products are usually semi-solid formulations, such as gels or creams, and generally include complex mixtures of different compounds, such as gelling or thickening agents, humectant agents and antimicrobial ingredients, which allow the product to be more easily spread on the site of application and also enhance their physicochemical and microbiological stability [1][2][3]. ...
Raman spectroscopy is a well-established technique for the molecular characterisation of samples and does not require extensive pre-analytical processing for complex cosmetic products. As an illustration of its potential, this study investigates the quantitative performance of Raman spectroscopy coupled with partial least squares regression (PLSR) for the analysis of Alginate nanoencapsulated Piperonyl Esters (ANC-PE) incorporated into a hydrogel. A total of 96 ANC-PE samples covering a 0.4% w/w–8.3% w/w PE concentration range have been prepared and analysed. Despite the complex formulation of the sample, the spectral features of the PE can be detected and used to quantify the concentrations. Using a leave-K-out cross-validation approach, samples were divided into a training set (n = 64) and a test set, samples that were previously unknown to the PLSR model (n = 32). The root mean square error of cross-validation (RMSECV) and prediction (RMSEP) was evaluated to be 0.142% (w/w PE) and 0.148% (w/w PE), respectively. The accuracy of the prediction model was further evaluated by the percent relative error calculated from the predicted concentration compared to the true value, yielding values of 3.58% for the training set and 3.67% for the test set. The outcome of the analysis demonstrated the analytical power of Raman to obtain label-free, non-destructive quantification of the active cosmetic ingredient, presently PE, in complex formulations, holding promise for future analytical quality control (AQC) applications in the cosmetics industry with rapid and consumable-free analysis.
... Conventional dermal formulations possess various limitations that include but are not limited to loss of dosage due to atmospheric deterioration, limited bioavailability (1.0−15%), and variation of release characteristics of the dried residue from the originally applied ones. 1 These formulations exhibit poor penetration abilities through the dead keratinized stratum corneum layer of the skin. 2 On the other hand, oral therapeutic administration can be a challenge for the disabled or elderly, young children, or unattainable for unconscious patients in a coma, while intravenous drug delivery carries the risk of infections and necessitates qualified people. 3 The alternative noninvasive approaches to transdermal drug delivery systems are envisaged as promising approaches to enhance and control drug transport across the skin, thus overcoming the aforementioned previous limitations while improving the safety and efficacy of marketed drugs. ...
Transdermal delivery is a potential alternative route to oral administration for drugs associated with stomach discomfort, such as flurbiprofen, a widely nonsteroidal anti-inflammatory drug (NSAID). This study aimed to design solid lipid nanoparticle (SLN) transdermal formulations of flurbiprofen. Chitosan-coated SLNs were prepared by the solvent emulsification method, and their properties and permeation profiles across the excised rat skin were characterized. The particle size of uncoated SLNs was at 695 ± 4.65 nm, which increased to 714 ± 6.13, 847 ± 5.38, and 900 ± 8.65 nm upon coating with 0.05, 0.10, and 0.20% of chitosan, respectively. The drug association efficiency was improved when a higher concentration of chitosan was employed over SLN droplets that endowed a higher affinity of flurbiprofen with chitosan. The drug release was significantly retarded as compared to the uncoated entities and followed non-Fickian anomalous diffusion that was depicted by "n" values of >0.5 and <1. Also, the total permeation of chitosan-coated SLNs (F7-F9) was significantly higher than that of the noncoated formulation (F5). Overall, this study has successfully designed a suitable carrier system of chitosan-coated SLNs that provide insight into the current conventional therapeutic approaches and suggest new directions for the advancements in transdermal drug delivery systems for improved permeation of flurbiprofen.
... Topical drugs are widely used for healing inflammatory skin diseases. One of the most commonly used topical drugs is the gel form due to its good drug release and cooling effect on the skin (Garg et al. 2015). ...
Nurani SG, Deluna NN, Nabila P, Falah S. 2022. Effectiveness of gel formulation of mahogany (Swietenia macrophylla) bark extract and its potential as an anti-inflammatory in white male rats (Rattus norvegicus). Nusantara Bioscience 14: 117-121. Mahogany bark contains phytochemical compounds that have anti-inflammatory activity. This study aims to determine the anti-inflammatory activity of gel formulation of mahogany bark extract in-vivo. Gel formulations of 96% ethanol extract of mahogany bark at different concentrations were tested for anti-inflammatory activity on the paws of rats induced by 1% carrageenan. The data observed were the thickness of the foot edema of rats. Positive control was anti-inflammatory drugs (Desoximetasone), and negative control was the gel formulation without extract. Data on the thickness of rat paw edema were analyzed using the ANOVA test. The results of the anti-inflammatory test showed that gel formulation 2 with an extract concentration of 10% had a thickness reduction value of 41.83%, which was not significantly different from the positive control treatment of 44.38%. The results of the dispersion test showed that formulation 2 and formulation 3 had good dispersibility as suggested in SNI, and all gel formulations had good adhesion. Based on these results, it was concluded that formulation 2 was the most effective in reducing rat paw edema.
... This is because creams are non-irritating, easily washable, and less greasy as compared to ointments. 23 The current findings conformed to studies conducted by Manju et al and Nerukar et al. 13,14 H1 antihistaminic drugs like levocetirizine (81.6%) were the most prescribed along with topical corticosteroids, followed by emollients (36.4%) and permethrin (29.2%). The reason for the high prescribing rates of antihistaminic drugs is the prevalence of itching as a non-specific symptom and antihistamines are believed to cause suppression of pruritus through decreased mast cell number and reduces tissue histamine levels. ...
Background: Topical corticosteroids form an important group of drugs in dermatology and are among the most commonly prescribed medications. However, despite their efficacy, they are associated with various adverse effects and as majority of the skin conditions are chronic, there is a need to ensure that there is rationality in drug use. Thus, this study was conducted with an aim to analyze the drug utilization pattern of topical corticosteroids.Methods: The study was a hospital-based, prospective and observational study and conducted for a period of 12 months. The method of data collection was done based on one-on-one consultation with patients. Data collected were recorded prospectively in a specially designed proforma. Results were then entered and analyzed using Microsoft excel.Results: In the study, it was observed that 48% of the patients were males while 52% were females. Most patients belonged to the age group of 21-30 years (30%). Scabies (30%) was the most common dermatological condition. With regard to the prescribing frequency of different topical corticosteroids, mometasone furoate (31.4%) was the preferred choice in most patients. H1 antihistaminic drugs like levocetirizine (81.6%) were the most prescribed along with topical corticosteroids, followed by emollients (36.4%) and permethrin (29.2%). The average number of drugs per prescription was 3.6 and all drugs were prescribed by their generic names.Conclusions: Periodic monitoring of the drug utilization pattern in the form of prescription auditing is an effective tool to constitute guidelines for improving the utilization pattern.
... Plant secondary metabolites with a pharmacological effect are used to develop topical formulations to deliver their effects into the skin for the treatment of local disorders [1]. For example, rosemary extract has shown antimicrobial activity in different cases [2][3][4][5][6]. ...
Rosmarinus officinalis belongs to the Lamiaceae family, and its constituents show antioxidant, anti-inflammatory, antidepressant, antinociceptive, and antibacterial properties. The aim of this study was to develop a topical formulation with R. officinalis extract that had antimicrobial and antioxidant activity. Maceration, infusion, Soxhlet, and ultrasound were used to produce rosemary extracts, which were submitted to antioxidant, compound quantification, cell viability, and antimicrobial assays. Infusion and Soxhlet showed better results in the DPPH assay. During compound quantification, infusion showed promising metabolite extraction in phenolic compounds and tannins, although maceration was able to extract more flavonoids. The infusion and ultrasound extracts affected more strains of skin bacteria in the disk diffusion assays. In the minimum inhibitory concentration assay, the infusion extract showed results against S. aureus, S. oralis, and P. aeruginosa, while ultrasound showed effects against those three bacteria and E. coli. The infusion extract was chosen to be incorporated into a green emulsion. The infusion extract promoted lower spreadability and appropriated the texture, and the blank formulation showed high levels of acceptance among the volunteers. According to the results, the rosemary extract showed promising antioxidant and antimicrobial activity, and the developed formulations containing this extract were stable for over 90 days and had acceptable characteristics, suggesting its potential use as a phytocosmetic. This paper reports the first attempt to produce an oil-in-water emulsion using only natural excipients and rosemary extract, which is a promising novelty, as similar products cannot be found on the market or in the scientific literature.
... Also, AuNPs provide antimicrobial action via ROS-independent pathways thereby stimulating angiogenesis and wound healing [174,175]. Likewise, ZnO NPs are antibacterial, anti-inflammatory, and antiseptic, and are frequently employed in the manufacture of skin creams, and ointments [176]. Due to their tiny size and high surface-to-volume ratio, ZnO exhibits greater Dendrimers Anti-inflammatory, increased production of transforming growth factor (TGF)-b1, interleukin (IL)-4 and IL-10, induced fibroblast proliferation, and gene therapy ...
Chronic wounds have been a global health threat over the past few decades, requiring urgent medical and research attention. The factors delaying the wound-healing process include obesity, stress, microbial infection, aging, edema, inadequate nutrition, poor oxygenation, diabetes, and implant complications. Biomaterials are being developed and fabricated to accelerate the healing of chronic wounds, including hydrogels, nanofibrous, composite, foam, spongy, bilayered, and trilayered scaffolds. Some recent advances in biomaterials development for healing both chronic and acute wounds are extensively compiled here. In addition, various properties of biomaterials for wound-healing applications and how they affect their performance are reviewed. Based on the recent literature, trilayered constructs appear to be a convincing candidate for the healing of chronic wounds and complete skin regeneration because they mimic the full thickness of skin: epidermis, dermis, and the hypodermis. This type of scaffold provides a dense superficial layer, a bioactive middle layer, and a porous lower layer to aid the wound-healing process. The hydrophilicity of scaffolds aids cell attachment, cell proliferation, and protein adhesion. Other scaffold characteristics such as porosity, biodegradability, mechanical properties, and gas permeability help with cell accommodation, proliferation, migration, differentiation, and the release of bioactive factors.
... Zinc is a necessary cofactor for metalloproteinase and for extracellular matrix and minerals (ECM). ZnO nanoparticles are commonly utilized in cosmetics, skin creams, and ointments because of their antibacterial, anti-inflammatory, and antiseptic qualities [121][122][123].The structure or amount of ZnO nanoparticles have an impact on wound healing. Because of its small size and high surface-to-volume ratio, ZnO has improved antibacterial activity. ...
Wounds are structural and functional disruptions of the skin that occur because of an accident. Chronic wounds are caused by a breakdown in the finely coordinated cascade of events that occurs during wound healing. Wound healing is a long process that split into at least three continuous and overlapping processes: an inflammatory response, a proliferative phase that leads to tissue repair, and third one is tissue remodeling. Therefore, wound healing studies are extensively studied to develop techniques that can achieve maximum recovery with minimum scar. Several growth hormones and cytokines secreted at the wound site tightly regulate wound healing processes. The traditional approach for wound management has been represented by topical treatments. Metal nanoparticles (e.g., silver, gold, zinc) are increasingly being employed in dermatology due to their favorable effects on wound healing, as well as in treating and preventing bacterial infections. The development of wound dressings materials has now been used to overcome the issues of external environments. The impregnated nanomaterials have provided moist environment that removes the exudates and avoid maceration. This review highlights the mechanism and focus on the current advancement of various nanoparticles impregnation material for wound healing process that can protect wound from infection and maintain the optimum exchange of gases.
... In light, developing topical platforms present attractive therapeutic aspects in terms of lower harm or incidence of serious adverse effects of systemically administered antifungal medications (oral or injectable), better efficacy and the ability to simply terminate the medication when necessary, hence, greater patient compliance (Estrada, 1987;Rezabek & Friedman, 1992). Indeed, effectiveness of any topically applied antifungal agent mainly depends on its concentration in the infected area, its activity spectrum and safety (Kalavathy et al., 2005;Garg et al., 2015). ...
Topical conveyance of antifungal agents like itraconazole ITZ has been giving good grounds for expecting felicitous antifungal medicines. The defiance of topical delivery of this poorly water soluble and high-molecular-weight drug, however, mightily entail an adequate vehiculation. ITZ aspasomes, newer antioxidant generation of liposomes, have been designed and enclosed in a cream to ameliorate skin deposition. The proposed creams containing non-formulated ITZ or encapsulated in aspasomes (0.1% or 0.5%) were topically applied in patients with diagnosed diaper dermatitis complicated by candidiasis, tinea corporis (TC), and tinea versicolor (TVC). Placebos (void aspasomal cream and cream base) were also utilized. The obtained results for diaper rash revealed that aspasomal cream (0.5% ITZ) was eminent with respect to complete cure and negative candida culture after 10-day therapy relative to counterparts containing 0.1% ITZ aspasomes or non-formulated ITZ (0.1% and 0.5%). For tinea, the same trend was manifested in terms of ‘cleared’ clinical response in 90% of patients and absence of fungal elements after 4-week treatment. Relative to non-formulated ITZ, ITZ aspasomal cream was endorsed to be auspicious especially when ITZ concentration was lowered to half commercially available cream concentration (1%), pushing further exploitation in other dermal fungal infections.
... Skin being the largest organ and the outermost layer of the human body is very much suited to targeted delivery of therapeutic agents through topical delivery [76]. This is because the human skin suffers from common diseases such as acne, wound, and other skin disorders [77]. The correct combination of active ingredients and base components would allow for a wide range of topical preparations suitable for delivering the active ingredients [76]. ...
Wound healing is a complex process driven by a series of stages that require a suitable wound closure environment, attributable to many factors. However, several factors contribute to delay in healing processes, including infection and the presence of certain diseases. Under unfortunate circumstances, an inadequate wound healing process could lead to amputation. Gauze is the traditional dressing to cover up wounds but tends to dry the wound bed. Therefore, a moist dressing may prove helpful in providing a suitable environment, preventing skin dryness, and enhancing angiogenesis of the wound area. The application of topical cream could expedite wound healing better than a moist dressing, as the former facilitates the repair process by maintaining the hydration levels of the affected skin. The issues mentioned above are discussed in detail in this review paper, focusing on recent advances, advantages and drawbacks of topical creams for wound treatment. In addition, the article includes suggestions to improve topical cream formulations for effective delivery of the needed therapeutic agents to assist in wound repair. Crucially, topical creams could play a key role in personal wound care and facilitate regenerative medicine. Novel strategies for speedy wound healing are in demand to alleviate the healthcare financial burden.
... Conventional dermal formulations possess various limitations that include but are not limited to loss of dosage due to atmospheric deterioration, limited bioavailability (1.0−15%), and variation of release characteristics of the dried residue from the originally applied ones. 1 These formulations exhibit poor penetration abilities through the dead keratinized stratum corneum layer of the skin. 2 On the other hand, oral therapeutic administration can be a challenge for the disabled or elderly, young children, or unattainable for unconscious patients in a coma, while intravenous drug delivery carries the risk of infections and necessitates qualified people. 3 The alternative noninvasive approaches to transdermal drug delivery systems are envisaged as promising approaches to enhance and control drug transport across the skin, thus overcoming the aforementioned previous limitations while improving the safety and efficacy of marketed drugs. ...
... Biliary salts were found to be less irritating, to have lower hemolytic activity and less protein release than other surfactants [40]. Gelling agents are used [41], since increasing solution viscosity may prolong the therapeutic effect of nasal preparations. However, increase the viscosity retards diffusion of drug from the matrix and may cause unwanted delay in drug absorption [42]. ...
Drug delivery by the intranasal route allows both systemic absorption and non-invasive brain targeting, due to the unique connection provided by the olfactory and trigeminal nerves between the brain and the external environment. Lipid nanocarriers can improve intranasal drug delivery by enhancing bioadhesion to nasal mucosa, and by protecting the encapsulated drug from biological degradation and transport efflux proteins. In this study two different biocompatible lipid nanocarriers were compared: nanoemulsions and solid lipid nanoparticles. The nasal uptake was investigated by labeling the nanocarriers lipid matrix with two fluorescent probes, 6-coumarin and rhodamine B, both lipophilic, yet characterized by different water solubility, in order to mimic the behavior of hypothetic drug compounds. Ex vivo permeation, in vivo pharmacokinetics and biodistribution studies were performed. 6-coumarin, water insoluble and therefore integral with the lipid matrix, was taken up to a limited extent, within a long timeframe, but with a proportionally more pronounced brain accumulation. In nanoemulsions soluble rhodamine B showed a relevant systemic uptake, with good bioavailability, likely due to the prompt release of the probe at the nasal mucosa.
... An ideal gel preparation should be sufficiently mobile in order to facilitate delivery of the dosage form to the application site yet adequately viscous to remain at the application site at an effective concentration [63,64]. The gel preparations in this work exhibited adequate viscosity ranging from 3355.00 ± 13.22 to 4519.67 ± 40.10 cP (i.e., within the typical viscosity range of~1000 cP to~100,000 cP when the gelling agents are used in a concentration of less than 10% [65]. ...
With the rising public awareness of environmental issues, consumers are increasingly demanding skin care products that create less environmental impact but still provide the same or even greater efficacy. In the skin care arena, microemulsions have been receiving increased attention as the promising delivery technology of skin care actives. Essential oils such as peppermint oil, lavender oil and eucalyptus oil are purported to have excellent antioxidant and antimicrobial properties that could be used as the eco-friendly alternatives for synthetic antioxidants and preservatives in the skin care formulations. This work therefore seeks to develop eco-friendly skin care formulations based on microemulsions of essential oil. Peppermint oil, lavender oil and eucalyptus oil were used as the oil phase to formulate naringin-loaded microemulsions, which demonstrated similar or better antioxidant and antimicrobial properties compared to the synthetic ones. When formulated into gel form, naringin-loaded microemulsion-gel formulations showed enhanced stability and release profile over their unformulated counterpart. Hence, microemulsions of essential oil developed in this work conferred a 4-fold benefits to the skin care formulations: (1) improved release (membrane permeation) of skin care active, (2) improved stability of skin care active, (3) as an eco-friendly alternative to synthetic antioxidant, and (4) a self-preserving system.
... To design the topical formulation, various delivery systems such as patches, pastes, creams, and ointments have been used (Garg et al., 2015). However, these all systems have several limitations. ...
To prepare a topical formulation of bimatoprost (BIM) with high skin permeability, we designed a solvent mixture system composed of ethanol, diethylene glycol monoethyl ether, cyclomethicone, and butylated hydroxyanisole, serving as a volatile solvent, nonvolatile co-solvent, spreading agent, and antioxidant, respectively. The ideal topical BIM formulation (BIM–TF#5) exhibited 4.60-fold higher human skin flux and a 529% increase in dermal drug deposition compared to BIM in ethanol. In addition, compared to the other formulations, BIM–TF#5 maximally activated human dermal papilla cell proliferation at a concentration of 5 μM BIM, equivalent to 10 μM minoxidil. Moreover, BIM–TF#5 (0.3% [w/w] BIM) significantly promoted hair regrowth in the androgenic alopecia mouse model and increased the area covered by hair at 10 days by 585% compared to the vehicle-treated mice, indicating that entire telogen area transitioned into the anagen phase. Furthermore, at day 14, the hair weight of mice treated with BIM–TF#5 (5% [w/w] BIM) was 8.45- and 1.30-fold greater than in the 5% (w/w) BIM in ethanol and 5% (w/v) minoxidil treated groups, respectively. In the histological examination, the number and diameter of hair follicles in the deep subcutis were significantly increased in the BIM–TF#5 (0.3 or 5% [w/w] BIM)-treated mice compared to the mice treated with vehicle or 5% (w/w) BIM in ethanol. Thus, our findings suggest that BIM–TF#5 is an effective formulation to treat scalp alopecia, as part of a novel therapeutic approach involving direct prostamide F2α receptor-mediated stimulation of dermal papilla cells within hair follicles.
... Focusing on the viscosity value of the hydrogels, which is a critical quality attribute, we can observe that all of them present a value coherent with the appropriate consistency for topical application, and in line with viscosities reported in the literature for topical formulation products [55]. ...
Topical delivery has received great attention due to its localized drug delivery, its patient compliance, and its low risk for side effects. Recent developments have focused on studying new drug delivery systems as a strategy for addressing the challenges of current topical treatments. Here we describe the advances on an innovative drug delivery platform called DELOS nanovesicles for topical drug delivery. Previously, the production of DELOS nanovesicles demonstrated potentiality for the topical treatment of complex wounds, achieving well-tolerated liquid dispersions by this route. Here, research efforts have been focused on designing these nanocarriers with the best skin tolerability to be applied even to damaged skin, and on exploring the feasibility of adapting the colloidal dispersions to a more suitable dosage form for topical application. Accordingly, these drug delivery systems have been efficiently evolved to a hydrogel using MethocelTM K4M, presenting proper stability and rheological properties. Further, the integrity of these nanocarriers when being gellified has been confirmed by cryo-transmission electron microscopy and by Förster resonance energy transfer analysis with fluorescent-labeled DELOS nanovesicles, which is a crucial characterization not widely reported in the literature. Additionally, in vitro experiments have shown that recombinant human Epidermal Growth Factor (rhEGF) protein integrated into gellified DELOS nanovesicles exhibits an enhanced bioactivity compared to the liquid form. Therefore, these studies suggest that such a drug delivery system is maintained unaltered when hydrogellified, becoming the DELOS nanovesicles-based hydrogels, an advanced formulation for topical use.
... Tapioca starch is particularly useful as it gives a very smooth feel to the product. Due to the chemically inert nature of talc and kaolin, they are the most commonly used ingredients in the formulation of dusting powder [104]. The presence of powders formed by spherical particles in formula allows an excellent spreadability increasing the duration and decreasing the transferability of the make-up. ...
The face powder was demanded by many nations in the world in the beginning AD and in Asia white skin was believed to be the sign of aristocratism, membership of the elite, and yet, white color is the pure symbol of the internal beauty and nobility. In addition, some face powders are sold in varying specialty shades to suit different skin needs; for example, a face powder with a greenish tinge will minimize the appearance of redness, while a purple-tinted powder may help the appearance of sallow or yellow skin. There is a legitimate reason to use face powder, and the pharmacopeias prescribe them in the treatment of many skin affections. At all events the proper use of powder is beneficial, it lightly covers and unifies a complexion, hiding the ravages of time, improving even the beautiful face. Face powder comes in different shades to match varying skin tones, and it is a good idea to choose the skin tone that most closely matches the natural skin. This will help the makeup appear more natural; it should be virtually unnoticeable. It may be necessary to use different face powders for summer and winter, as the skin may become tanner in the summer, or drier and in need of extra moisture in the winter. They are of benefit in acne, freckles, sunburn and red nose. Beneath their attractive aspect and odor, face powders should be made by the perfumer to combine the qualities of an elegant cosmetic and therapeutic agent; they must primarily possess adherence, lightness and be transparent; secondly, they should be detergent and delicately absorbent in order to aid the natural functions of the skin, taking up the fatty matters not easily dislodged by water; they should also tend to increase the natural elasticity and regular functions of the skin.
... The choice of a specific dosage form is an essential parameter because it can affect the absorption and the bioavailability of the bioactives as a function of interactions that can occur between excipients and biological barriers (i.e., skin, mucosae and intestinal epithelium), and between excipients and bioactives. Different types of dosage forms and excipients can be used to maximize the beneficial effect of bioactives depending on the target, the characteristics of the bioactives, and the administration route (Garg et al., 2015). ...
Plants and their derivates have been used as medicines for centuries and today is being re-discovered their usefulness for the human health. The therapeutic properties of phytochemicals are re-evaluated under the light of medical and pharmacological research, pushed by a constantly growing market demand, where consumers trust more natural products than synthetic drugs. New studies are enlightening the effectiveness of phytochemicals against a wide range of ailments, nevertheless very few evaluate the efficacy of topical formulations based on natural bioactive molecules in the treatment of nasal mucosal diseases.
This review aims at exploring this little covered topic. An overview on the properties and functionality of the nasal mucosa and the different diseases affecting it has been provided. We summarized various nasal dosage forms containing natural bioactive and explored how innovative delivery systems loading phytochemicals can improve the treatment results. Finally, the potential use of novel nanocarriers for the treatment of nasal ailments has been covered as well.
... In general, nanotechnology offers a better controlled, nontoxic, more secure and localized delivery of drugs than traditional treatments. A variety of nanotechnology colloidal carriers are popular for treating and controlling psoriasis because of their distinctive characteristics, such as liposomes, niosomes, transmitters, microspheres, micelles, dendrimers, glycosomes, solid lipid nanoparticles, etc. (Figure 3) [70][71][72][73][74][75][76][77][78]. ...
Psoriasis is a genetic chronic disease mediated by the immune system with systemic and cutaneous manifestations that can significantly deteriorate patients’ quality of life. Two–three percent of the population worldwide suffer from psoriasis and it imposes a substantial economic burden on patients. The aetiology is mainly related with genes and environmental factors. The pathophysiology of psoriasis is characterized by T cells and dendritic cells, antimicrobial peptides, genetic predispositions, lipoprotein-2, galactosin-3, fractalkine, vaspin, and human neutrophilic peptides, etc. in the progression of psoriasis. For patients with psoriasis, the traditional treatments include corticosteroids, vitamin D3
analogues, calcineurin inhibitors, methotrexate, cyclosporine, acitretin, phototherapy, and biological agents, etc. Nanodermatology is an emerging, multidisciplinary science that is gaining increasing recognition in the treatment of psoriasis. This review provides a summary of the pathophysiology, epidemiology, clinical diagnosis, and classical pharmacotherapy of psoriasis. The review also summarizes different nanotechnology therapies for effective treatment of psoriasis.
... This allows their non-problematic application by the dentist or by the patient while ensuring the relatively quick release of the drug at the site of application. Their main advantage is a low risk of irritation [112], as well as good rheological properties and good adhesion to differentiated oral mucosa [113]. ...
The success of modern dental treatment is strongly dependent on the materials used both temporarily and permanently. Among all dental materials, polymers are a very important class with a wide spectrum of applications. This review aims to provide a state-of-the-art overview of the recent advances in the field of natural polymers used to maintain or restore oral health. It focuses on the properties of the most common proteins and polysaccharides of natural origin in terms of meeting the specific biological requirements in the increasingly demanding field of modern dentistry. The use of naturally derived polymers in different dental specialties for preventive and therapeutic purposes has been discussed. The major fields of application cover caries and the management of periodontal diseases , the fabrication of membranes and scaffolds for the regeneration of dental structures, the manufacturing of oral appliances and dentures as well as providing systems for oral drug delivery. This paper also includes a comparative characteristic of natural and synthetic dental polymers. Finally, the current review highlights new perspectives, possible future advancements, as well as challenges that may be encountered by researchers in the field of dental applications of polymers of natural origin.
Background: Despite recent advances in wound healing products, phytochemicals have been considered promising and attractive alternatives. Carvacrol (CAR), a natural phenolic compound, has been reported to be effective in wound healing.
Purpose: This work endeavored to develop novel CAR-loaded phytosomes for the enhancement of the wound healing process.
Methods: Molecular docking was performed to compare the affinities of the different types of phospholipids to CAR. Phytosomes were prepared by three methods (thin-film hydration, cosolvency, and salting out) using Lipoid S100 and Phospholipon 90H with three levels of saturation percent (0%, 50%, and 100%), and three levels of phospholipid molar percent (66.67%, 75%, and 80%). The optimization was performed using Design Expert where particle size, polydispersity index, and zeta potential were chosen as dependent variables. The optimized formula (F1) was further investigated regarding entrapment efficiency, TEM, 1H-NMR, FT-IR, DSC, X-RD, in vitro release, ex vivo permeation, and stability. Furthermore, it was incorporated into a hydrogel formulation, and an in vivo study was conducted to investigate the wound-healing properties of F1.
Results: F1 was chosen as the optimized formula prepared via the thin-film hydration method with a saturation percent and a phospholipid molar percent of zero and 66.67, respectively. TEM revealed the spherical shape of phytosomal vesicles with uniform size, while the results of 1H-NMR, FT-IR, DSC, and X-RD confirmed the formation of the phytosomal complex. F1 demonstrated a higher in vitro release and a slower permeation than free CAR. The wound area of F1-treated animals showed a marked reduction associated with a high degree of collagen fiber deposition and enhanced cellular proliferation.
Conclusion: F1 can be considered as a promising remedy for the enhancement of wound healing and hence it would be hoped to undergo further investigation.
Neurodegenerative diseases are a significant cause of mortality worldwide, and the blood-brain barrier (BBB) poses a significant challenge for drug delivery. An intranasal route is a prominent approach among the various methods to bypass the BBB. There are different pathways involved in intranasal drug delivery. The drawbacks of this method include mucociliary clearance, enzymatic degradation and poor drug permeation. Novel nanoformulations and intranasal drug-delivery devices offer promising solutions to overcome these challenges. Nanoformulations include polymeric nanoparticles, lipid-based nanoparticles, microspheres, liposomes and noisomes. Additionally, intranasal devices could be utilized to enhance drug-delivery efficacy. Therefore, intranasal drug-delivery systems show potential for treating neurodegenerative diseases through trigeminal or olfactory pathways, which can significantly improve patient outcomes.
Kulit yang sering terpapar sinar matahari dan polusi memerlukan perawatan dengan produk yang mampu melindungi dari paparan radiasi UV dan radikal bebas. Biji buah alpukat diketahui memiliki potensi sebagai tabir surya dan aktivitas antioksidan yang baik. Penelitian ini bertujuan untuk membuktikan aktivitas antioksidan dan tabir surya ekstrak aseton biji buah alpukat, menghasilkan formula krim yang memiliki fungsi sebagai tabir surya dan antioksidan bagi kulit, serta mengetahui korelasi konsentrasi ekstrak dengan aktivitas tabir surya krim ekstrak aseton biji alpukat. Pengujian aktivitas tabir surya dan antioksidan dilakukan secara in vitro. Hasil penelitian menunjukan nilai SPF dan IC50 ekstrak berturut-turut 39,636 dan 10,36 ppm. Nilai SPF krim F1, F2 dan F3 berturut-turut 1,859±0,152, 2,941±0,065 dan 3,629±0,053. Nilai SPF krim ketiga formula berbeda bermakna (p<0,05) dan terdapat korelasi signifikan (p<0,001) dan kuat antara konsentrasi ekstrak dengan nilai SPF. Nilai IC50 krim formula F1, F2 dan F3 berturut-turut 9,74 ppm, 7,02 ppm dan 6,86 ppm. Berdasarkan hasil tersebut dapat disimpulkan ekstrak aseton biji alpukat memiliki aktivitas tabir surya tingkat proteksi tinggi dan aktivitas antioksidan sangat kuat. Krim memiliki nilai SPF di bawah kategori tingkat proteksi rendah dan aktivitas antioksidan sangat kuat. Terdapat korelasi bermakna dan kuat antara konsentrasi ekstrak dengan nilai SPF krim.
In the present work, sandwich-like polycaprolactone/gelatin/polycaprolactone electrospun multilayered mats were implemented to control the release of the water-soluble drug such as ceftazidime (CTZ). The outer layers were made from polycaprolactone nanofibers (NFs), and CTZ-loaded gelatin provided an internal layer. The release profile of CTZ from mats was compared with monolayer gelatin mats and chemically cross-linked GEL mats. All the constructs were characterized using scanning electron microscopy (SEM), mechanical properties, viscosity, electrical conductivity, X-ray diffraction (XRD), and Fourier transform-infrared spectroscopy (FT-IR). In vitro cytotoxicity against normal fibroblasts as well as antibacterial activity of CTZ-loaded sandwich-like NFs were investigated by the MTT assay. The results showed that the drug release rate from the polycaprolactone/gelatin/polycaprolactone mat was slower than that of gelatin monolayer NFs, and the rate of release can be adjusted by changing the thickness of hydrophobic layers. The NFs exhibited high activity against Pseudomonas aeruginosa and Staphylococcus aureus, while no significant cytotoxicity was observed against human normal cells. Altogether, the final mat as a predominant antibacterial scaffold can be used for controlled drug release of water-soluble drugs as the wound healing dressings in tissue engineering.
Gum is a plant-based substance that, when combined with water, creates a thick, sticky solution or gel. Chemically, they are polysaccharides. Some of their characteristics, including plentiful abundance, biodegradability, nontoxicity, and low price, make them more useful in the commercial food and pharmaceutical industries than synthetic polymers. Holy basil (Ocimum sanctum) is a culinary herb of the Labiatae family, with over 150 species in the genus Ocimum. The seed-gum of Ocimum is a complex polysaccharide. It is mostly constituted of d-xylose (35%), d-galacturonic acid (28%), l-arabinose (21%), and l-rhamnose (16%), with traces of galactose and glucose. It has a lengthy, branched (1 → 4) linked xylan backbone in its polysaccharide chain. Protein solubility, syneresis, foaming efficiency, foaming stability, emulsification efficiency, emulsification stability, pH, total dietary fiber, insoluble dietary fiber, soluble dietary fiber, viscosity, and sticking temperature are all physical parameters that have been reported. The qualities of emulsification action, sticky properties, foaming stability, gel formation, viscosity, surface-active activity, and high stabilization demonstrate their usefulness in the processing of functional foods and dairy-derived products. Its capacity to disintegrate and entrap drugs as a polymer matrix is important for innovative drug delivery methods. As a fat substitute, basil seed gum (BSG) is employed in dairy and functional foods to retain their stability, texture, taste, and other organoleptic features. According to a thorough analysis of the literature, basil seed gum has several biological actions such as antibacterial, prebiotic, antioxidant, shelf-life enhancer, antidiabetic, cholesterol, and bile acid-binding. The most recent scientific research on basil seed gum’s chemical, physical, and biological characteristics and uses is gathered from a range of research papers in this study.
Atraric acid (AA) is a phenolic compound isolated from Stereocaulon japonicum that has demonsstarted anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system composed of ethanol as a volatile vehicle, oleic acid as a permeation enhancer, and water for skin hydration. The ideal topical AA formulation (AA–TF#15) exhibited 8.77-fold higher human skin flux and 570% increase in dermal drug deposition, compared to 1% (w/w) AA in ethanol. In addition, compared to other formulations, AA–TF#15 (1% [w/w] AA) activated keratinocytes and human dermal papilla cell proliferation at a concentration of 50 µM AA, which is equivalent to 50 µM minoxidil. Moreover, AA–TF#15 treatment produced a significant increase in hair regrowth by 58.0% and 41.9% compared to the 1% (w/w) minoxidil and oral finasteride (1 mg/kg)-treated mice. In addition, AA–TF#15 showed a higher expression level of aldehyde dehydrogenase 1, β-catenin, cyclin D1, and pyruvate kinase M2 proteins in the skin of AA–TF#15-treated mice compared to that of those treated with minoxidil and oral finasteride. These findings suggest AA–TF#15 is an effective formulation for the treatment of scalp androgenic alopecia.
Moisturizers are one of the most widely used preparations in cosmetics and have been extensively used to soften the skin for consumers. Moisturizers work effectively in combating dry skin which may cause pain, tightness, itch, stinging, and/or tingling. The aim of this review is to evaluate published studies on the history, ingredients, preparation processes, characteristics, uses, and applications of moisturizers. Moisturizers bridge the gap between medicine and consumer goods by being used to make the skin more beautiful and healthy. In the future, in moisturizer therapy, the capacity to adapt specific agents to specific dermatological demands will be crucial. Cosmetically, moisturizers make the skin smooth by the mechanism of increasing the water content in the stratum corneum, hence exerting its most vital action, which is moisturizing action and maintaining a normal skin pH.
Computer-based modeling and simulation is emerging as a useful tool to complement the analysis and interpretation of biological data. The large volume, scale, and complexity of data generated from in vitro, in vivo, and ex vivo data cannot be analyzed and interpreted by conventional data analysis tools. So, various in silico computational e-resources, databases, and simulation softwares are being used for the determination of pharmacokinetic (PK) and pharmacodynamic (PD) parameters for the management of diseases. These tools help in providing multiscale representation of the biological processes in the order of increasing complexity from that of protein and genes, cells, isolated tissues and organs, and the whole organism. The United States Food and Drug Administration (USFDA) has also directed the use of PK/PD simulation for the evaluation of drugs during the clinical phase, in which the primary focus is on the establishment of relationship between therapeutic drug concentration and patient response. The aim of this chapter is to discuss the role, advancement, and development of biocomputational tools used in research and development in the pharmaceutical industry, wherein the number of experimental studies is exponentially growing. Furthermore, application of these studies to optimize the dosing regimens, dose-response relationship, etc. will be discussed.KeywordsBiomolecular simulationIn silico modelingPharmacokineticPharmacodynamic simulation
Medicines are often mixtures comprising active pharmaceutical ingredients (APIs) and excipients, components that usually bulk up formulation or stabilize APIs. The need for therapeutic potential enhancements of APIs with poor solubility and permeability or for their targeted delivery requires more complex formulations. Polymers belong to a class of pharmaceutical excipients that are often used as API (drug) carriers. The advancement in the design of polymers and synthesis methods allows the control of drug delivery either via improving drug dissolution, aiding the drug diffusion, or degradation of the carrier matrix at the site of action. These mechanisms depend on the structures of formulation components and importantly on their intermolecular interactions. The structure elucidation of polymers is often impeded by their nature and lack of homogeneity, while the experimental evaluation of intermolecular interactions provides limited information. That information at the atomistic level can be obtained by using computational chemistry. The focus of this chapter is on the in silico approaches to generate three-dimensional models of drugs and polymers and evaluate interactions between them as a basis for the rational design of pharmaceutical formulations.
This chapter reviews the basic concepts involved in topically applied pharmaceuticals for local delivery as well as transdermal delivery. The principle of transdermal drug delivery system is to deliver drug through the skin in a controlled and predetermined rate for systemic action while dermal drug delivery is intended for local action. Stratum corneum, the upper layer of the skin plays a pivotal role as rate-limiting barrier in drug permeation. The chapter discusses how the drug permeates through the skin. Semisolid preparations for dermal drug delivery i.e., ointments and creams are discussed in detail since these are common conventional dosage forms administered topically. Moreover, transdermal patches and microneedles are also explained in this chapter.
Objective Topical application of ambonese banana (Musa paradisiaca var. sapientum (L.) kuntze) stem sap gel (GEGPA) on the socket wound area showed an increase in the expression of platelet-derived growth factor-BB, while decrease in the expression of matrix metalloproteinase-2 and 9. The aim of this study is to achieve standard formulation of GEGPA through stability, viscosity, distribution area, and drugs release for oral gel wound healing.
Materials and Methods This is an in vitro and in vivo study with the randomized posttest only control group design. The gel was formulated according to the composition of each group by adding hydroxypropyl methylcellulose (HPMC), Lexgard, propylene glycol, and cold water to obtain 100 g of gel. Observations were made through the following tests: stability, viscosity, distribution area, drug release, and histopathological analysis of tooth extraction wound healing.
Statistical analysis Data were analyzed using a one-way analysis of variance (α = 0.05) with GraphPad Prism-8 statistical software.
Results The study showed that the GEGPA formulation was stable against changes in consistency, color, smell, homogeneity, and pH value. There is a significant difference between groups with respect to viscosity (p = 0.0001), adhesion (p = 0.004), dispersion (p = 0.000), and fibroblast cell numbers on days 3 and 5 (p = 0.007 and p = 0.001). There is no interaction between the active ingredients and the gel base of all formulations. Formulation 3 had better properties in terms of viscosity, broad distribution, and drug release compared with other groups. Application of GEGPA to tooth extraction wounds showed a significant proliferation of fibroblast cells on days 3 and 5.
Conclusions The formulation of M. paradisiaca var. sapientum (L.) kuntze extract with HPMC and propylene glycol obtained a gel preparation, GEGPA, that was organoleptically stable and met the topical gel standard for wounds in the oral cavity.
The paper is a compilation of varied excipients currently employed in the manufacturing of different dosage forms. Advancements in drug delivery can be accomplished only with accomplishments in excipient industry by way of isolating, extracting or synthesizing newer excipients of plant and/or synthetic origin with biodegradable and/or biocompatible properties, designing tailor made excipients for specific dosage forms either in the cosmeceutical, nutraceutical or drug delivery systems for varied routes of administration embedded with QbDparadigmns, or envisioned newer techniques viz., the principles of green chemistry. Despite such remarkable achievements in the excipient industry, drug interactions, packaging incompatabilities are inevitable. The future of this industry is poignantly decisive on striking a chord between the two. An excipient is stated to be defined by Beena P et al as"A substance formulated alongside the active ingredient of a medication, included for long-term stabilization, bulking up solid formulations that contain potent active ingredients in small amounts (that are often referred to as bulking agents, fillers, or diluents), or to grant a therapeutic enhancement on the active ingredient in the final dosage form, such as facilitating drug absorption, reducing viscosity, or enhancing solubility" 1. Another definition stated excipients to be "A pharmacologically dynamic medication or pro-drug which are incorporate into the assembling procedure or are contained in a completed pharmaceutical item measurements form" 2. Many excipients have envisaged numerous applications in the pharmaceutical industry, especially in the manufacturing process where its appropriate selection is brusquely governed by a myriad of factors-the routes of administration, the nature and type of dosage forms and the delivery systems, the physio-chemical properties of the active ingredients, etc. that inadvertently converged onto a "structure-property-application" paradigm.
The concept of “one size fits all” followed by the conventional healthcare system has drawbacks in providing precise pharmacotherapy due to variation in the pharmacokinetics of different patients leading to serious consequences such as side effects. In this regard, digital-based three-dimensional printing (3DP), which refers to fabricating 3D printed pharmaceutical dosage forms with variable geometry in a layer-by-layer fashion, has become one of the most powerful and innovative tools in fabricating “personalized medicine” to cater to the need of therapeutic benefits for patients to the maximum extent. This is achieved due to the tremendous potential of 3DP in tailoring various drug delivery systems (DDS) in terms of size, shape, drug loading, and drug release. In addition, 3DP has a huge impact on special populations including pediatrics, geriatrics, and pregnant women with unique or frequently changing medical needs. The areas covered in the present article are as follows: (i) the difference between traditional and 3DP manufacturing tool, (ii) the basic processing steps involved in 3DP, (iii) common 3DP methods with their pros and cons, (iv) various DDS fabricated by 3DP till date with discussing few research studies in each class of DDS, (v) the drug loading principles into 3D printed dosage forms, and (vi) regulatory compliance.
AIM: To explore the effects of liniment levamisole on cellular immune functions of patients with chronic hepatitis B.
METHODS: The levels of T lymphocyte subsets and mIL-2R in peripheral blood mononuclear cells (PBMCs) were measured by biotin-streptavidin (BSA) technique in patients with chronic hepatitis B before and after the treatment with liniment levamisole.
RESULTS: After one course of treatment with liniment levamisole, the levels of CD3⁺, CD4⁺, and the ratio of CD4⁺/CD8⁺ increased as compared to those before the treatment but the level of CD8⁺ decreased. The total expression level of mIL-2R in PBMCs increased before and after the treatment with liniment levamisole.
CONCLUSION: Liniment levamisole may reinforce cellular immune functions of patients with chronic hepatitis B.
Keywords: Liniment levamisole, Chronic hepatitis B, Cellular immune function, T lymphocyte subsets, mIL-2R
Citation: Wang KX, Zhang LH, Peng JL, Liang Y, Wang XF, Zhi H, Wang XX, Geng HX. Effect of liniment levamisole on cellular immune functions of patients with chronic hepatitis B. World J Gastroenterol 2005; 11(45): 7208-7210
The choice of an optimum constructional material for the electrosurgical cutting tools based on nanostructured crystals of partially stabilized zirconia (NPSZe) is substantiated on the basis of criteria of operational stability and functional efficiency. The results of research into adsorption of organic molecules on the surface of the material are used to study the adhesion characteristics of NPSZe. The models of the innovative tools, such as curved bipolar electrosurgical scissors, bipolar forceps, tweezers, and dissectors with nonstick spray, are presented. An experimental model of a high-frequency generator necessary for optimal tool operation is considered.
Psoriasis is an autoimmune, chronic, inflammatory skin disease characterized by epidermal hyperplasia, proliferation of blood vessels, and infiltration of leukocytes in dermis and epidermis. Several immunosuppressants such as methotrexate (MXT) and cyclosporine are used but they are associated with adverse effects due to down regulation of immune system. Numerous approaches have been explored to overcome the problems of conventional topical system such as high frequency of application, impermeability to skin barrier, and limited efficacy. Photodynamic therapy is another non-invasive technique currently used for skin diseases. The combination of two drugs is also commonly observed to achieve more effective therapy. In the present study, antipsoriatic activity of niosomal formulations for the treatment of psoriasis in combination with narrow and broad band UV radiation had been explored in experimental animal model.
Significance
Topical prevention of HIV is designed to pharmacologically interrupt sexual transmission at the genital mucosa. Attempts at preventing transmission in women using vaginal gels have yielded disappointing results in part because of poor rates of adherence. Controlled topical drug delivery using intravaginal ring technology should improve efficacy and adherence by providing sustained mucosal delivery of antiretrovirals. In this paper, we describe a reservoir intravaginal ring that delivers tenofovir disoproxil fumarate (TDF) for 1 month. The ring protected pigtailed macaques from weekly vaginal simian–human immunodeficiency virus challenges for 4 mo. The sterilizing performance of this drug delivery system supports the concept that an intravaginal ring delivering TDF could be an effective tool for prevention of HIV sexual transmission in women.
Background:
Trials of a vaginal Tenofovir gel for pre-exposure prophylaxis (PrEP) for HIV have given conflicting results. Knowledge of concentrations of Tenofovir and its active form Tenofovir diphosphate, at putative sites of anti-HIV functioning, is central to understanding trial outcomes and design of products and dosage regimens. Topical Tenofovir delivery to the vaginal environment is complex, multivariate and non-linear; determinants relate to drug, vehicle, dosage regimen, and environment. Experimental PK methods cannot yield mechanistic understanding of this process, and have uncontrolled variability in drug sampling. Mechanistic modeling of the process could help delineate its determinants, and be a tool in design and interpretation of products and trials.
Methods and findings:
We created a four-compartment mass transport model for Tenofovir delivery by a gel: gel, epithelium, stroma, blood. Transport was diffusion-driven in vaginal compartments; blood concentration was time-varying but homogeneous. Parameters for the model derived from in vitro and in vivo PK data, to which model predictions gave good agreement. Steep concentration gradients occurred in stroma ≤ 8 hours after gel release. Increasing epithelial thickness delayed initial TFV delivery to stroma and its decline: tmax increased but AUC at 24 hours was not significantly altered. At 24 and 48 hours, stromal concentrations were 6.3% and 0.2% of C(max). Concentrations in simulated biopsies overestimated stromal concentrations, as much as ∼5X, depending upon time of sampling, biopsy thickness and epithelial thickness.
Conclusions:
There was reasonably good agreement of model predictions with clinical PK data. Conversion of TFV to TFV-DP was not included, but PK data suggest a linear relationship between them. Thus contrasts predicted by this model can inform design of gels and dosage regimens in clinical trials, and interpretation of PK data. This mass transport based approach can be extended to TFV conversion to TFV-DP, and to other drugs and dosage forms.
Iontophoresis was used to enhance the delivery of aceclofenac (ACF) from topical gels formulated with various polymers for the purpose of relieving pain and inflammation.
Gels were formulated from hydroxypropyl methyl cellulose (HPMC), carbopol 934P, and sodium carboxymethyl cellulose (NaCMC). The formulations were evaluated for cathodal iontophoretic delivery of ACF through excised rat abdominal skin at three levels of current density of 0.5, 0.6 and 0.7 mA/cm(2). The in vivo effectiveness of the drug delivered passively as well as under the influence of iontophoresis at pH 7.4 at a current density of 0.5 mA/cm(2) was also investigated using male Albino rats with carrageenan induced paw edema.
In the ex vivo studies, though it was clear that iontophoresis significantly increased drug permeation through the excised skin from all formulations; the percentage drug permeated from HPMC gels was superior to that from carbopol 934P or NaCMC gels but increased with an increase in the current density only for the former. The steady state flux, permeability coefficient, enhancement factor were significantly greater from HPMC gels than from the gels of the ionic polymers due to the interference of competitive ions. With iontophoresis, the carrageenan induced paw edema was significantly reduced by 61.53% (P < 0.01) for HPMC gels as compared to the control although passive permeation without iontophoresis showed a 54.6% reduction (P < 0.05) at the end of 4 h.
The results of the study indicate that ACF could be administered topically by using iontophoresis from a suitably formulated gel for effective control of pain and inflammation.
Cetirizine is a piperazine-derived second-generation antihistaminic drug recommended for treatment of pruritus associated with atopic dermatitis. The present investigation encompasses development of a nanosized novel elastic vesicle-based topical formulation of cetirizine dihydrochloride using combination of Phospholipon® 90G and edge activators with an aim to have targeted peripheral H1 antihistaminic activity. The formulation was optimized with respect to phospholipid/drug/charge inducer ratio along with type and concentration of edge activator. The optimized formulation was found to be satisfactory with respect to stability, drug content, entrapment efficiency, pH, viscosity, vesicular size, spreadability, and morphological characteristics. The ex vivo permeation studies through mice skin were performed using Franz diffusion cell assembly. It was found that the mean cumulative percentage amount permeated in 8 h was almost twice (60.001 ± 0.332) as compared to conventional cream (33.268 ± 0.795) and aqueous solution of drug (32.616 ± 0.969), suggesting better penetration and permeation of cetirizine from the novel vesicular delivery system. Further, therapeutic efficacy of optimized formulation was assessed against oxazolone-induced atopic dermatitis in mice. It was observed that the developed formulation was highly efficacious in reducing the itching score (4.75 itches per 20 min) compared to conventional cream (9.75 itches per 20 min) with profound reduction in dermal eosinophil count and erythema score. To conclude, a novel vesicular, dermally safe, and nontoxic topical formulation of cetirizine was successfully developed and may be used to treat atopic dermatitis after clinical investigation.
Abstract Dermatological inflammatory diseases often affect the scalp and the eyebrows. Common dosage forms available on the market for those situations are lotions; however, the presence of hair limits their use. Gels, for their consistency and adhesiveness, are a suitable alternative to the lotions in these situations. The aim of this study was to develop a new stable gel containing mometasone furoate (MF), with anti-inflammatory activity and a controlled delivery, to improve topical treatment of scalp dermatitis. Pharmaceutical development, physical and chemical characterization, stability, in vitro release and permeation studies and in vivo anti-inflammatory activity were performed. The gel presented an acidic pH and an apparent viscosity of 35 Pa.s. The microbiological analysis showed that the results were within the established specification limits. The release and the permeation profiles suggest that the drug is mainly retained in the upper skin layers. MF gel was tested in an animal model of cutaneous inflammation and presented similar anti-inflammatory activity compared to a commercially available MF dosage form. The gel was chemically, physically and microbiologically stable. The results suggest that the developed hydrogel formulation containing MF can be of actual value for improving the clinical effectiveness in the treatment of scalp dermatitis.
The Unani eye drop is an ophthalmic formulation prepared for its beneficial effects in the inflammatory and allergic conditions of the eyes. In the present study, the Unani eye drop formulation was prepared and investigated for its anti-inflammatory and antihistaminic activity, using in vivo and in vitro experimental models respectively. The Unani eye drop formulation exhibited significant anti-inflammatory activity in turpentine liniment-induced ocular inflammation in rabbits. The preparation also showed antihistaminic activity in isolated guinea-pig ileum. The anti-inflammatory and antihistaminic activity of eye drop may be due to presence of active ingredients in the formulation. Although there are many drugs in Unani repository which are mentioned in classical books or used in Unani clinical practice effectively in treatment of eye diseases by various Unani physicians. Inspite of the availability of vast literature, there is a dearth of commercial Unani ocular preparations. So, keeping this in mind, the eye drop formulation was prepared and its anti-inflammatory and antihistaminic activity was carried out in animal models. Thus, in view of the importance of alternative anti-inflammatory and antiallergic drugs, it becomes imperative to bring these indigenous drugs to the front foot and evaluate their activities.
Epithelial tissue provides the body with its first layer of protection against harmful environmental stimuli by enacting the regulatory interplay between a physical barrier preventing the influx of external stimuli and an inflammatory response to the infiltrating stimuli. Importantly, this interdependent regulation occurs on different time scales: the tissue-level barrier permeability is regulated over the course of hours, whereas the cellular-level enzymatic reactions leading to inflammation take place within minutes. This multi-scale regulation is key to the epithelium's function and its dysfunction leads to various diseases. This paper presents a mathematical model of regulatory mechanisms in the epidermal epithelium that includes processes on two different time scales at the cellular and tissue levels. We use this model to investigate the essential regulatory interactions between epidermal barrier integrity and skin inflammation and how their dysfunction leads to atopic dermatitis (AD). Our model exhibits a structure of dual (positive and negative) control at both cellular and tissue levels. We also determined how the variation induced by well-known risk factors for AD can break the balance of the dual control. Our model analysis based on time-scale separation suggests that each risk factor leads to qualitatively different dynamic behaviours of different severity for AD, and that the coincidence of multiple risk factors dramatically increases the fragility of the epithelium's function. The proposed mathematical framework should also be applicable to other inflammatory diseases that have similar time-scale separation and control architectures.
A hypersensitivity reaction, either anaphylactic or anaphylactoid, is a well-known adverse effect following intravenous and oral administration of vancomycin. The authors report a case of circulatory collapse and its management after the topical application of vancomycin powder during spinal instrumentation surgery. A 52-year-old woman with breast cancer and metastasis to her spine underwent a vertebrectomy of the T-10 vertebra with instrumented reconstruction from T-8 to T-12. The patient was hemodynamically stable during most of the procedure despite a 2-L blood loss requiring administration of crystalloids, colloids, packed red blood cells, and fresh-frozen plasma. During closure of the subcutaneous layer, there was a sudden drop in blood pressure from 120/60 to 30/15 mm Hg and an increase in heart rate from 95 to 105 bpm. No skin erythema or rash was visible, and there was no bronchospasm or increase in airway pressure. The patient was treated with fluids, boluses of ephedrine, phenylephrine, and adrenaline. The operation was completed and the patient woke up neurologically intact but did require blood pressure support with a norepinephrine infusion for the next 4 hours. She was discharged from hospital in a good clinical state on the 4th postoperative day. It was speculated that the rapid absorption of vancomycin powder applied on the surgical wound caused an anaphylactoid reaction and the circulatory collapse. With an increase in the use of topical vancomycin in surgical wounds, communication and awareness among all intraoperative team members is important for rapid diagnosis of an adverse reaction and for appropriate management.
Date syrup as a nutritional additive and safe alternative to added sugar is one of the best choices for milk flavoring. In this study, a flavored milk beverage was formulated using date syrup for flavoring the product and gum tragacanth to obtain an acceptable mouth feel. Steady shear and dynamic oscillatory rheological properties of the samples contained 3 concentrations (0, 0.1, 0.2, and 0.3%, wt/wt) of 2 types of gum tragacanth (Astragalus gossypinus andAstragalus rahensis) which at 3°C, were studied. Particle size distribution and colorimetric assays were determined by laser diffractometry and using reflection spectrometer, respectively. Sensory analysis was performed with 25 semitrained panelists, using a 5-point hedonic scale. The results showed that viscoelastic properties, flow behavior parameters, particle size, and color parameters (L*, a*, and b*, where L* represents lightness, a* represents the redness/greenness quality of the color, and b* represents the yellowness and blueness quality of the colors) were significantly affected by the concentration of the gum tragacanth and the severity of this effect was influenced by the type of gum. The use of appropriate type and concentration of gum tragacanth in date milk formulation can improve the texture and mouth feel by affecting on particle size and the flow behavior of this product.
Heating a methylcellulose solution forms a thermal-reversible hydrogel. After the hydrogel forms, its properties change according to its temperature. However, the effects of heating this solution during storage and then cooling it are unclear. We investigated the effects of this heating and cooling on rheological and drug release characteristics. We prepared samples of methylcellulose solution (2% methylcellulose and 20% D-sorbitol) and examined them under two conditions: 1) storage for 24 hours at 4 to 30℃, 2) storage for 24 hours at 4 to 50℃, then cooling to 4℃ and maintained for 4 hours. We performed rheological investigations of viscosity, gelation temperature and gel strength, and examined the drug release characteristics by using a diffusion cell method with acetaminophen as the model drug. It was found that as the storage temperature rose, the methylcellulose solution increased in viscosity and the gelation temperature and gel strength changed. During storage at 30℃, the amount of drug released by the solution increased and the diffusion coefficient was high. When cooled to 4℃, the solution recovered its viscosity, gelation temperature, gel strength and drug release characteristics, regardless of the previous storage temperature. These results clarify that although the rheological and drug release characteristics of methylcellulose solution change with changes in storage temperature, the original characteristics are recovered after the solution is cooled to 4℃ and maintained at that temperature for four hours.
This article presents the development and evaluation of a new topical formulation of diclofenac diethylamine (DDA) as a locally applied analgesic lotion.
To this end, the lotion formulations were formulated with equal volume of varying concentrations (1%, 2%, 3%, 4%; v/v) of permeation enhancers, namely propylene glycol (PG) and turpentine oil (TO). These lotions were subjected to physical studies (pH, viscosity, spreadability, homogeneity, and accelerated stability), in vitro permeation, in vivo animal studies and sensatory perception testing. In vitro permeation of DDA from lotion formulations was evaluated across polydimethylsiloxane membrane and rabbit skin using Franz cells.
It was found that PG and TO content influenced the permeation of DDA across model membranes with the lotion containing 4% v/v PG and TO content showed maximum permeation enhancement of DDA. The flux values for L4 were 1.20±0.02 μg.cm(-2).min(-1) and 0.67 ± 0.02 μg.cm(-2).min(-1) for polydimethylsiloxane and rabbit skin, respectively. Flux values were significantly different (p < 0.05) from that of the control. The flux enhancement ratio of DDA from L4 was 31.6-fold and 4.8-fold for polydimethylsiloxane and rabbit skin, respectively. In the in vivo animal testing, lotion with 4% v/v enhancer content showed maximum anti-inflammatory and analgesic effect without inducing any irritation. Sensatory perception tests involving healthy volunteers rated the formulations between 3 and 4 (values ranging between -4 to +4, indicating a range of very bad to excellent, respectively).
It was concluded that the DDA lotion containing 4% v/v PG and TO exhibit the best performance overall and that this specific formulation should be the basis for further clinical investigations.
The isoflavone genistein (GEN) is a natural product with potential applications for skin cancer treatment and chemoprevention; however its high lipophilicity and chemical instability limits its clinical use. Therefore, attempts towards protecting GEN against degradation and increasing its penetration in the skin might be a valid approach. In this work, GEN loaded-PLA nanocapsules (GEN-NC) were prepared by interfacial deposition of preformed polymer (nanoprecipitation); physicochemical characterization and stability studies for 90 days were conducted. GEN-NC were incorporated into semi-solid formulations and permeation experiments were carried out using porcine ear skin. GEN-NC optimized formulation presented a mean diameter of 139 +/- 7.31 nm, polydispersity index of 0.128 +/- 0.08, encapsulation efficiency of 89.63 +/- 2.27% and drug loading from 0.6 to 1.4 w/w%. Stability studies demonstrated that nanocapsules did not exhibit aggregation during the 90 days of the assay, however, a drop in encapsulation efficiency was observed in the first 10 days. Permeation experiments demonstrated that a higher amount of GEN reaches deeper layers of the skin and increased penetration was achieved when GEN-NC were incorporated in a semi-solid gel formulation, indicating that GEN-NC might be a promising nanocarrier system for skin delivery of GEN.
Thermosensitive hydrogel containing drug-loaded liposomes delivery system offers the possibility of reduced dosing frequency and sustained drug action. In the study, a soluble chitosan derivative, N-[(2-hydroxy-3-trimethylammonium) propyl] chitosan chloride, was used and interacted with glycerophosphate to produce a thermosensitive hydrogel as the matrix of doxorubicin-loaded liposomes. The formulation could retain the liquid state with good fluidity below or at room temperature for long time but turn into a nonflowing gel after exposing to body temperature for no more than 5 min. The mean size of liposomes was increased when dispersed into the hydrogel, while the entrapment efficiency of doxorubicin in liposomes was not discounted by the hydrogel, which was over 90%. The in vitro release experiment performed with a dialysis membrane model showed that the liposomes-containing hydrogel exhibited an excellent sustained-release behavior, which eliminated the initial burst release occuring in the liposomal formulation and only released about 22% loaded drug in 9 days. In vivo antitumor activity was evaluated by the survival time of H22-bearing mice treated with various doxorubicin formulation, which showed that the hydrogel enhanced the antitumor activity and reduced the systemic toxicity. Thus, all these results demonstrated that the thermosensitive hydrogel with embedded liposomes is a promising antitumor drug carrier for topical cancer therapy.
Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and modify pharmacokinetic and bio-availability. Topically applied niosomes can increase the residence time of drugs in the stratum corneum and epidermis, while reducing the systemic absorption of the drug. It can act as drug containing reservoirs and the modification of the vesicular compositions or surface properties can adjust the drug release rate and the affinity for the target site. Ketoconazole is a broad spectrum Imidazole derivative useful in the treatment of superficial and systemic fungal infections.
In order to improve the low skin penetration and to minimize the side effects associated with topical conventional drug administration, Ketoconazole niosomes were prepared by a thin film hydration method using different ratios of non-ionic surfactants (Span 40, 60 and Tween 60) along with cholesterol (CHO). The formulations were evaluated for size, shape, entrapment efficiency and in vitro drug release.
Niosomes appeared spherical in shape and size range was found to be 4.86 ± 1.24-7.38 ± 3.64 μm. The entrapment efficiency was found in the range of 55.14 ± 2.29-78.63 ± 0.91% and in vitro drug release in the range of 46.63 ± 0.95-72.37 ± 0.59% in 24 h. Ketoconazole niosomes formulated with Span 60 and CHO in the ratio of 1:0.2 were found to be promising and were incorporated into 1% Carbopol gel. The formulated gel was evaluated for various physicochemical parameters and antifungal activity. The in vitro drug release study was carried out using phosphate buffer saline pH 7.4 and was found to be 36.18 ± 1.50% in 12 h.
Gel formulation containing niosomes loaded with Ketoconazole showed prolonged action than formulations containing Ketoconazole in non-niosomal form and it can be developed successfully to improve the antifungal activity.
Physicochemical properties of chiral ibuprofen are significant to formulation scientists because its enantiomers and eutectics possess lower melting points than its racemate. The influence of these properties on transdermal formulation development, especially the relative effect of lowered melting point, on skin permeation must be carefully assessed to provide the most efficacious formulation. Thermodynamic properties and crystalline structures of the enantiomers, eutectics, and racemate of chiral ibuprofen were investigated by differential scanning calorimetry and X-ray powder diffraction. The effect of melting point lowering on membrane permeation rates was mathematically modeled. Model was validated by in vitro skin permeation experiments using different preparations of racemic ibuprofen, enantiomer, and eutectic. Both enantiomer and eutectic formed a two-phase liquid system containing an emulsifiable aqueous phase and an oily phase in the presence of aqueous isopropyl alcohol (aIPA). The eutectic emulsion had the highest permeation rate, a 2.21-fold increase in flux compared with saturated aIPA solutions of the racemate with a 2.03-fold increase in flux. Results from the two-phase liquid system supported those from the mathematical models, albeit somewhat lower, and confirmed their use in predicting maximum flux utilizing thermodynamic data. Study data also supported the idea that eutectic formation, for ibuprofen and probably other chiral drugs, may be one of the best ways to develop topical formulations for improved percutaneous absorption to avoid the use of permeation enhancers or synthetically modifying chemical structure. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
To evaluate the antifungal activity of four honeys of different types from Algeria against pathogenic yeast i.e. Candida albicans (C. albicans) and Rhodotorula sp.
Four Algeria honeys of different botanical origin were analyzed to test antifungal effect against C. albicans, and Rhodotorula sp. Different concentrations (undiluted, 10%, 30%, 50% and 70% w/v) of honey were studied in vitro for their antifugal activity using C. albicans and Rhodotorula sp. as fungal strains.
The range of the diameter of zone of inhibition of various concentrations of tested honeys was (7-23 mm) for Rhodotorula sp., while C. albicans showed clearly resistance towards all concentrations used. The MICs of tested honey concentrations against C. albicans and Rhodotorula sp. were (70.09-93.48)% and (4.90-99.70)% v/v, respectively.
This study demonstrates that, in vitro, these natural products have clearly an antifungal activity against Rhodotorula sp. and C. albicans.
To evaluate the additive action of ginger starch on the antifungal activity of honey against Candida albicans (C. albicans).
C. albicans was used to determine the minimum inhibitory concentration (MIC) of four varieties of Algerian honey. Lower concentrations of honey than the MIC were incubated with a set of concentrations of starch and then added to media to determine the minimum additive inhibitory concentration (MAIC).
The MIC for the four varieties of honey without starch against C. albicans ranged between 38% and 42% (v/v). When starch was incubated with honey and then added to media, a MIC drop was noticed with each variety. MAIC of the four varieties ranged between 32% honey (v/v) with 4% starch and 36% honey (v/v) with 2% starch.
The use of ginger starch allows honey benefit and will constitute an alternative way against the resistance to antifungal agents.
Ultrapotent topical corticosteroids are the mainstay of psoriasis treatment, used either alone or in combination with a topical vitamin D analog. Traditionally used in an ointment vehicle for psoriasis, clobetasol propionate 0.05% is also available in spray, foam, lotion, and shampoo formulations, which may provide for improved convenience and acceptance in many patients with similar efficacy, safety, and tolerability as the traditional ointment and cream formulations. To compare newer formulations with traditional ointment and cream formulations, we performed a systematic review of the literature. Search terms included 'clobetasol propionate,' combination with 'psoriasis,' 'vasoconstriction,' ' vasoconstrictor,' or 'absorption' for each of the four vehicles ('spray,' 'foam,' 'lotion,' and 'shampoo'). While there are very few direct comparison studies between clobetasol propionate in different vehicles, the efficacy rates (with success defined as clear or almost clear of psoriasis) for more recent formulations are high, with most patients achieving success after 2-4 weeks of treatment in well controlled clinical trials, with response rates that are similar to those with the traditional clobetasol propionate ointment. Small differences in vasoconstrictor potency or cutaneous absorption have been noted among the formulations, but the clinical significance of these observations is difficult to discern. Recent research has emphasized the importance of treatment adherence in the management of psoriasis. Adherence to treatment is likely to be a far more important determinant of success than are small differences in drug delivery, especially in actual clinical use as opposed to the well controlled environment of clinical trials. For patients who prefer a less messy vehicle, adherence and outcomes are likely to be better with the more recent formulations compared with the traditionally recommended ointment.
Cycloferon, a prospective interferon inductor, and the mechanism of its action were characterized. Its formulation for external use as liniment was developed. The pharmacotherapeutic effect of the drug in the treatment of paradontitis was shown. The drug efficacy in herpetic lesions of the mouth and lips mucosa was observed. The use of cycloferon in the treatment of the buccal mucosa affections in HIV-infected subjects was substantiated.
The aim of the study was to estimate the efficacy of liniment cycloferon included in combined therapy of herpetic infection in 30 patients with psoriasis divided into 2 groups. Combined treatment of patients with recurrent herpetic infection promoted elimination of general infection syndrome, shortened duration of eruption and local inflammation, accelerated epithelization of herpetic erosion, and decreased the frequency of relapses during the follow-up.
The efficiency of cycloferon liniment in combined treatment of herpetic infection in patients with latent form of HIV infection has been assess by observations of 40 patients divided into two groups. In the first group, the standard treatment was supplemented with the application of cycloferon liniment twice a day during 7 days; in the second group, the therapy was conducted according to standard recommendations. It was established that the application of cycloferon liniment in combination with standard therapy in patients with relapse of herpetic infection against the background of HIV infection ensures faster disappearance of general infectious syndrome, decreases the period of eruptions and the duration of local inflammations, and accelerates the epithelialization of erosions.
We characterised biological properties of novel formulations of two low-potency glucocorticosteroids, dexamethasone and hydrocortisone, which have an equivalent dose ratio of 1:50 in vasoconstriction tests. The rate of such carrier-mediated, mainly non-diffusive glucocorticosteroids transport with very deformable lipid vesicles (Transfersomes®) through the skin, and the corresponding cutaneous drug biodistribution data, were complemented with the drug bio-efficacy studies. The minimum effective drug dose that reduces arachidonic acid-induced murine ear oedema by 50% was used as one bioactivity indicator. The minimum drug amount ensuring such an effect in mouse skin decreases appreciably when a corticosteroid is applied epicutaneously with very deformable vesicles rather than a lotion or a crème. Specifically, the minimum effective dose for hydrocortisone in very deformable carriers is 2–3 μg cm−2 whereas for the crème- or lotion-like preparations at least 10 μg cm−2 is required. Such three- to fivefold relative increase of hydrocortisone potency is accompanied by at least 13%, and more often >20%, absolute drug potency enhancement. The delivery of hydrocortisone with very deformable carriers moreover prolongs the suppression of the drug-induced oedema nearly 2-fold (to ∼24 h per application). The effective dose of dexamethasone delivered with very deformable vesicles into murine skin is reduced >10 times compared with the crème- or lotion-based products. Specifically, less than 0.1 μg cm−2 dexamethasone in very deformable vesicles suppresses the arachidonic acid-induced murine ear oedema >50%, on the average. Dexamethasone use on the skin in such vesicles extends the duration of drug action fourfold, compared with a commercial crème, i.e. to >48 h per application. Epicutaneous use of glucocorticosteroids in very deformable vesicles also diminishes such drug's abrasion sensitivity and may increase the general robustness of drug effect. Lower frequency of skin treatment, which ensures adequate biological response, is a result of this. Topical corticosteroid delivery with very deformable vesicles, Transfersomes®, thus improves the therapeutic risk–benefit ratio, arguably due to better targeting into and longer drug presence in the skin.
Abstract The clinical use of halobetasol propionate (HP) is related to some adverse effects like irritation, pruritus and stinging. The purpose of this work was to construct HP-loaded solid lipid nanoparticles (HP-SLN) formulation with skin targeting to minimizing the adverse side effects and providing a controlled release. HP-SLN were prepared by solvent injection method and formula was optimized by the application of 3(2) factorial design. The nanoparticulate dispersion was evaluated for particle size and entrapment efficiency (EE). Optimized batch was characterized for differential scanning calorimetry (DSC), scanning electron microscopy, X-ray diffraction study and finally incorporated into polymeric gels of carbopol for convenient application. The nanoparticulate gels were evaluated comparatively with the commercial product with respect to ex-vivo skin permeation and deposition study on human cadaver skins and finally skin irritation study. HP-SLN showed average size between 200 nm and 84-94% EE. DSC studies revealed no drug-excipient incompatibility and amorphous dispersed of HP in SLN. Ex vivo study of HP-SLN loaded gel exhibited prolonged drug release up to 12 h where as in vitro drug deposition and skin irritation studies showed that HP-SLN formulation can avoid the systemic uptake, better accumulative uptake of the drug and nonirritant to the skin compared to marketed formulation. These results indicate that the studied HP-SLN formulation represent a promising carrier for topical delivery of HP, having controlled drug release, and potential of skin targeting with no skin irritation.
Chitosan, a β-1,4-linked polymer of glucosamine with lesser amounts of N-acetylglucosamine, has well-recognized hemostatic properties. Chitosan is also able to open tight cellular junctions, facilitating paracellular drug transport and delivery. Chitosan, through topical application, facilitates the systemic delivery of analgesic drugs. Theoretically this ability could be used to enhance the local delivery of hemostatic drugs, such as tranexamic acid, improving chitosan's role as a topical dressing. Individually a chitosan-dextran gel and tranexamic acid have been shown to improve hemostasis after endoscopic sinus surgery. A combination of both should lead to improved hemostasis and better postsurgical outcomes. The use of a chitosan/tranexamic acid dressing could have a wide range of potential beneficial applications in a number of other clinical surgical settings. While the initial main application might be as an improved external hemostatic dressing, it should also be useful on a range of internal surgical wounds.
Assessment of skin uptake and clearance are important to determine the efficiency and systemic safety of dermatological formulations. The objective of this study was to assess the skin uptake, clearance and possible systemic delivery of ciclopirox following topical application in wistar rats. In vitro studies (3 h) were carried out in excised pig skin to assess the permeation and retention capacity of ciclopirox in skin layers using gel formulations (1 and 2% w/v). In vivo dermatopharmacokinetics (DPK) parameters were determined by measuring the drug levels in the skin as a function of time post application (0.5, 1, 1.5 and 2 h) and post removal (3, 4, 6 and 8 h) of the formulation in wistar rats. The plasma drug concentrations were also determined in same animals. In vitro data indicates low permeability and high retention of ciclopirox in the stratum corneum. DPK data observed indicate higher Cmax value (175.43 ± 25.62 µg/cm(2) ) and AUC (632.14 ± 102.26 µg.h/cm(2) ) with 2% (w/v) gel formulation. Further, the skin elimination of ciclopirox follows first order kinetics with a short half-life (t1/2 ~2 h). The fraction of drug reaching systemic circulation was found to be significantly low (~0.15% of the applied dose). A relation between the drug concentration in the skin layers and the plasma was observed with a short lag period. The topical availability of ciclopirox was found to be relatively low and endured rapid clearance with minimal systemic uptake. This article is protected by copyright. All rights reserved.
Abstract The aim of this study was to develop liposomal-based (LBGF) and micro-emulsion-based (MBGF) gel formulations of croconazole to compare their topical delivery potential. Conventional gels were also prepared using various polymers such as sodium carboxymethyl cellulose (SCMC), Poloxamer 407, Carbopol 971P and chitosan. The in vitro release of croconazole from conventional gel formulations, LBGF and MBGF were carried out using cellophane membrane as permeation membrane. However, in vitro skin permeations studies of all formulations were carried out using rat skin. The results of the drug release/skin permeation studies indicated that the highest release was obtained from SCMC followed by chitosan, Poloxamer 407 and finally Carbopol 971P gel. Therefore, liposomes and micro-emulsions were loaded on Carbopol 971P gel. The drug release and skin permeation of croconazole from different LBGF and MBGF showed that MBGF had superior release/permeation than LBGF. MBGF having ethanol as co-surfactant showed higher release/permeation of drug than MBGF-containing propylene glycol. The analysis of data according to different kinetic models indicated that the release of drug from different LBGF and MBGF followed the Higuchi model. The antimicrobial activity of the different LBGF and MBGF of croconazole was carried out by measuring the inhibition zone (mm) and compared by the effect of miconazole cream as control. The different LBGF and MBGF showed an excellent activity against different species of fungi as compared with miconazole cream. Overall, these results indicated that developed LBGF and MBGF could have great potential for topical delivery of croconazole.
The incidence of methicillin-resistant Staphylococcus aureus (MRSA) infection has significantly increased. Generally, the success of this bacterium as a pathogen is attributed to its ability to adhere to surfaces and remain there, under the protection of an extracellular matrix known as biofilm. To combat MRSA with regular doses of vancomycin, efforts are continuously underway to increase its effectiveness. A promising technique is to