Article

Comprehensive review on additives of topical dosage forms for drug delivery

Taylor & Francis
Drug Delivery
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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.

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... 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. ...
Article
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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.
... Several formulations are seen to be used in the topical route delivery such as foams, sprays, medicated powders, and solution. 1 Topical drug delivery system is increasingly becoming more popular and useful in the dermatological field -this is because the penetration of many drug substances is affected by the skin since it acts as a mechanical barrier and delivers medicine both consistently and locally. The affordability and ease of use of the epidermis make it highly popular. ...
... 3 1.1. Advantages of topical delivery system 1 ...
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Tinea infections are one of the most occurring dermatophyte infection in the world and more so in tropical countries. It majorly infect children which may lead to them being segregated and shunned away from the community thereby affecting their psychological state. To prepare topical gel containing deep eutectic mixture of luliconazole heating and dispersion method were utilised, and it comprised several steps. The main focus was to improve the solubility as well as the permeability of the drug as it comes into contact with the skin. Choline bitartrate was used as a hydrogen bond donor (HBD), Gallic acid which is a carboxylic acid was used as a hydrogen bond acceptor (HBA), Carbopol 984NF a carbomer was used as a gelling agent. A combination of choline bitartrate and gallic acid in the ratio expressed by formulation code N3 was used for the final preparation. The final properties of the gel; viscosity, spreadability and the drug release profile of the prepared gel were investigated. The drug release of the prepared formulation was compared to the marketed formulation. 4 formulations were prepared using different ratios of the excipients and the optimized formulations were subjected to characterization. Viscosity of the tablet was controlled by amount of gelling agent used in the manufacturing process. Following FTIR studies, it was found that there were no interaction between the drug and the excipients and that the drug release depended on the type of the excipients used in the formulation. Dispersion method was found to be a suitable, easy and efficient technique for designing Topical gel containing deep eutectic mixture (DEM) for topical use.
... 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] . ...
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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. ...
Article
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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.
... 29 Generally, water-in-oil and oil-inwater forms ointment and creams respectively and can influence the overall scalability of the process. 30 Although, the production of cream and corresponding oil:water ratio and texture variability could not be controlled in small-scale batch production at our laboratory, the applicability (API incorporation) was not compromised. Anionic, cationic and nonionic materials are generally used as emulsifying agents based on certain criteria, especially those associated with the stability of the APIs intended to be incorporated into the base material. ...
... Many topical preparations were applied on the skin; locally and transdermal delivery system, can be found as (Figure-2): solid like dusting powder (antifungal powder), semisolid like: ointment (lidocaine®), cream (Fucidin®), gel (Reparile®), lotion (Calamina®) and liquid (Canstine® solution) in addition to spray (Angiovage®), foam (vaginal wash foam), transdermal and microneedle patch (16) . ...
Article
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In general; many approaches found to delivered the drug to the site of action, one of these approaches used the skin barrier as a rout to reach the drug to the local or systemic targeting; Both local and transdermal drug product are intended for external use (applied on the skin). It was localized action on one or more layers of the skin, or may reach to the systemic circulation to get systemic effect. So, in this review authors aimed to highlight on the anatomy of the skin layers epidermis, dermis and hypodermis (to know the way of the drug transport), drug application, drug penetration through the skin, factors affecting on the skin drug absorption, advantage of this rout and limitation of the drug delivery system; in addition to mention to many examples of this dosage forms are used in drug delivery system. Finally, this approach of drug delivery system is widely used and preferred from the patient at any life stages because of its improved the patient compliance and decreased the side effects of drugs in addition to easy rout of admiration and avoid pain and suitable to patient with swallowed problem.
... Wool fat, shea butter, isopropyl myristate, and medium-chain triglycerides are procured from Croda. All other chemicals used in the study were of analytical grade purchased from Merck and Co. Demineralized water was employed for the formulation development study [11][12][13][14]. ...
Article
Vitamin C is extensively used in cosmetic formulation, howbeit stability is the supreme demerit that limits its use in beautifying products. Numerous techniques are being employed to inhibit the degradation of vitamin C caused by formulation components to facilitate the use in skin rejuvenating products. Diverse materials are being exercised in formulation to stabilize the ascorbic acid and ingredients selected in this formulation composition help for stabilization. The initial stable prototype is developed and further optimization is accomplished by applying the design of experiment tools. The stable pharmaceutical formulations were evaluated for the evaluation parameters and designated as two optimized formulations. The analytical method for the assay of ascorbic acid from the United States pharmacopeia and the related substance method from European pharmacopeia has been modified to be used for cream formulation. The DoE design exhibited that the stability of formulation is impacted by citric acid and tartaric acid but not by propylene glycol and glycerin. The analysis results of topical formulations for the evaluation parameter exhibited satisfactory results. The in-vitro release study method has been developed, optimized, and validated to fit the analysis. The in-vitro studies have been performed for selected compositions and both the formulation has similar kinds of release patterns. The stability study as per ICH guidelines exhibited that the product is stable for accelerated, intermediate, and room-temperature storage conditions. The optimized formulation shows constant release and permeation of ascorbic acid through the skin. The formulation with the combinations of citric acid, tartaric acid, and tocopherol is more stable and the degradation of vitamin C has been reduced significantly. The beaucoup strategies in the unique composition help to protect the degradation by inhibiting the multitudinous degradation pathways.
... Topical dosage formulation enhancers are mostly used to manage absorption, maintain consistency, improve stability and organoleptic properties, and increase formulation volume. Topical formulations facilitate the delivery of biologically active substances to the site of action as well as increased bioavailability of encapsulated medicinal components [3] . ...
... The proposed system, which integrates nanotechnology-based delivery systems, sustained release formulations, targeted drug delivery approaches, personalized medicine, and artificial intelligence, offers promising avenues for overcoming existing limitations and enhancing therapeutic outcomes [12] . By leveraging these innovative approaches, researchers and pharmaceutical scientists can develop customized formulations tailored to individual patient profiles, optimize drug release kinetics, and enhance targeting efficiency, ultimately improving patient adherence, safety, and efficacy. ...
... Semisolid topical dosage forms including creams, lotions, or ointments have stickiness, stability issues, and poor spreadability or permeability compared to others because of their high solid contents and the presence of mixtures of oil phases compromising their stability during storage. 17,18 To this end, gels are a relatively newer class of dosage form that have marked applications by circumventing these limitations. Hydrogels are semisolid three-dimensional cross-linked polymeric networks that can imbibe a huge volume of water and undergo swelling or shrinkage to facilitate controlled drug-release. ...
Article
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Skin is the largest organ of the human body, as it protects the body from the external environment. Nowadays, skin diseases and skin problems are more common, and millions of people are affected daily. Skin diseases are due to numerous infectious pathogens or inflammatory conditions. The increasing demand for theoretical research and practical applications has led to the rising prominence of gel as a semisolid material. To this end, organogels has been widely explored due to their unique composition, which includes organic solvents and mineral or vegetable oils, among others. Organogels can be described as semisolid systems wherein an organic liquid phase is confined within a three-dimensional framework consisting of self-assembled, cross-linked, or entangled gelator fibers. These gels have the ability to undergo significant expansion and retain substantial amounts of the liquid phase, reaching up to 99% swelling capacity. Furthermore, they respond to a range of physical and chemical stimuli, including temperature, light, pH, and mechanical deformation. Notably, due to their distinctive properties, they have aroused significant interest in a variety of practical applications. Organogels favor the significant encapsulation and enhanced permeation of hydrophobic molecules when compared with hydrogels. Accordingly, organogels are characterized into lecithin organogels, pluronic lecithin organogels, sorbitan monostearate-based organogels, and eudragit organogels, among others, based on the nature of their network and the solvent system. Lecithin organogels contain lecithin (natural and safe as a living cell component) as an organogelator. It acts as a good penetration enhancer. In this review, first we have summarized the fundamental concepts related to the elemental structure of organogels, including their various forms, distinctive features, methods of manufacture, and diverse applications. Nonetheless, this review also sheds light on the delivery of therapeutic molecules entrapped in the lecithin organogel system into deep tissue for the management of skin diseases and provides a synopsis of their clinical applications.
... Topical drug delivery is an effective, targeted, and popular therapy for local dermatological disorders because it avoids the first-pass effect, gastrointestinal irritation, and metabolic degradation associated with oral administration (Shrestha et al., 2017;Garg et al., 2015). Topical routes provide high therapeutic efficacy along with a more beneficial profile of adverse effects than in regular systematic application, especially for analgesic drugs like lidocaine and capsaicin in patches, capsaicin creams, or emulgels (Leppert et al., 2018). ...
Article
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Topical therapy with emulgel-type of products allows efficient delivery of bioactive compounds with additional benefits to patients. This research aimed to design, optimize, formulate, and evaluate in vitro parameters between gels loaded with a microemulsion of extracted capsaicin to their standard. A crude form of capsaicin was extracted from capsicum. Using Box Behnken design, 15 different microemulsions were made by ultrasonication and optimized by varying three independent variables (amount of olive oil, Hydrophilic-lipophilic balance value of surfactants, and amount of surfactants used) using Stagraphic Centurion software. Microemulsions were optimized based on their organoleptic characters; dilution test, centrifugation test and P H , and gelling agent Carbopol-940 was determined by its viscosity, spreadability, swelling index, consistency, and P H. Finally, a stable capsaicin emulgel (0.05% and 0.1%) was made by incorporating optimized microemulsion (F8) and optimized gelling agent, 0.6% Carbopol-940. Those final capsaicin emulgels were tested for drug content percentage, which was within the standard range.
... There are various pharmaceutical dosage forms that can be used for wound care. Topical dosage forms, such as liquids, semi-solids, transdermals, plasters, and film-forming sprays, tend to be used [31,32]. Topical drugs remain critical to treating all wound types by accelerating the wound healing process and reducing infection risk. ...
Article
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Objective: Proper wound care is essential to prevent complications and worsening of the injured patient. Everyone in the family needs to possess wound care knowledge, especially the mother, who plays a role in making decisions about health care and family health behaviors. This study aims to evaluate mothers' knowledge towards wound care in the Greater Bandung Area. Methods: This cross-sectional study involved 100 participants with varied backgrounds and had met the inclusion criteria. The study was conducted using questionnaires distributed online to the mother community living in the Greater Bandung Area, West Java, then data processing and analysis were carried out. Results: The results showed that mothers in the Greater Bandung Area had a good level of knowledge (27%), average (52%), and less (21%). In addition, plasters with wound care solutions were still the mothers' main choice in wound care. Nevertheless, there are many choices of pharmaceutical dosage forms for wound care that have been developed today to optimize the wound healing process. Conclusion: Most of the mothers already have an average level of knowledge to good. However, there are still quite a lot of mothers who have a lack of knowledge related to wound care. Therefore, educational programs must be developed to raise awareness about wound care and management, as well as knowledge about pharmaceutical dosage forms for wound care.
... 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. ...
Article
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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]. ...
Article
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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. ...
Article
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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). ...
Article
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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]. ...
Article
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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]. ...
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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. ...
Article
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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.
... Chemically, natural gums are complex carbohydrates in which one or more types of monosaccharide units such as arabinose, galactose, glucose, mannose, xylose, or uronic acid are joined by hydroxyl groups and glycosyl bonds to create a macromolecular structure [19]. Gums are used as a bulking agent, disintegrant, binder, suspending agent, coating agent, emulsifier, stabilizer, laxative, sustained release agent, demulcent, emollient, mucoadhesive agent, and filmforming agent in pharmaceuticals [19][20][21][22][23]. Basil seeds have been utilized in traditional medicine to relieve stress, reduce weight, reduce inflammation, indigestion, constipation, ulcers, diarrhea, diuretics, antipyretics, and other ailments [24,25]. ...
Chapter
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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.
... 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). ...
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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. ...
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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]. ...
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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.
... Chemically, natural gums are complex carbohydrates in which one or more types of monosaccharide units such as arabinose, galactose, glucose, mannose, xylose, or uronic acid are joined by hydroxyl groups and glycosyl bonds to create a macromolecular structure [19]. Gums are used as a bulking agent, disintegrant, binder, suspending agent, coating agent, emulsifier, stabilizer, laxative, sustained release agent, demulcent, emollient, mucoadhesive agent, and filmforming agent in pharmaceuticals [19][20][21][22][23]. Basil seeds have been utilized in traditional medicine to relieve stress, reduce weight, reduce inflammation, indigestion, constipation, ulcers, diarrhea, diuretics, antipyretics, and other ailments [24,25]. ...
... 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 ...
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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. ...
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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.
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Current treatments for severe acne include combinations of synthetic anti-inflammatory and antibacterial drugs, which possess numerous side effects. Therefore, this study developed microemulsion-based hydrogel containing lemongrass leaf essential oil (Cymbopogon citratus (DC.) Stapf) and mango seed kernel extract (Mangifera indica Linn) as a potential natural therapy for inflammatory acne. To this end, the microemulsions were first prepared using pseudo-ternary phase diagrams with soybean oil and coconut oil, cremophor RH40, and PEG 400. The optimal formula could load 1% lemongrass oil and 10% mango extract, possessed a spherical droplet size of ~18.98 nm, a zeta potential of -5.56 mV, and a thermodynamic stability. Secondly, the microemulsion-based hydrogel was developed by simple mixing the optimal microemulsion in carbopol-940 hydrogel (3.5% w/w). The product showed a viscosity of ~3728 cPs, a pH of 5.4-6.2, a spreadability of ~24 cm, an in-vitro Franz-cell cumulative release rate of ~80% for polyphenol content and ~60% for citral within 12 h, and a good physicochemical stability of > 3 months. Thirdly, the skin compatibility/irritability of the microemulsion-based hydrogel was determined by the HET-CAM assay, which showed non-irritation level. Finally, the anti-inflammatory activities of the hydrogel, using heat-induced BSA denaturation assay and LPS-stimulated RAW 264.7 NO inhibition assay, was 4-times higher than that of the reference drug Klenzit-C® (adapalene and clindamycin gel). Moreover, the hydrogel possessed strong anti-biofilm activity in Cutibacterium acnes, comparable with Klenzit-C®. Conclusively, the microemulsion-based hydrogel containing lemongrass oil and mango seed extract demonstrated much potentials to be a promising natural drug for acne treatment.
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Addressing infectious conditions presents a formidable challenge, primarily due to the escalating issue of bacterial resistance. This, coupled with limited financial resources and stagnant antibiotic research, compounds the antibiotic crisis. Innovative strategies, including novel antibiotic development and alternative solutions, are crucial to combat microbial resistance. Nanotherapeutics offers a promising approach to enhance drug delivery systems. Integration into lipid-based nanoscale delivery systems, particularly through therapeutic substance encapsulation in liposomal carriers, significantly prolongs drug presence at infection sites. This not only reduces toxicity but also shields antibiotics from degradation. Lipidic carriers, particularly liposomes, exhibit remarkable specificity in targeting infectious cells. This holds great promise in combating antimicrobial resistance and potentially transforming treatment for multi-drug resistant infections. Leveraging liposomal carriers may lead to breakthroughs in addressing drugresistant bacterial infections. This review emphasizes the potential of antimicrobial-loaded liposomes as a novel delivery system for bacterial infections. Encapsulating antimicrobial agents within liposomes enhances treatment efficiency. Moreover, liposomal systems counteract challenges posed by antimicrobial resistance, offering hope in managing persistent multidrug-resistant infections. In the battle against bacterial resistance and the antibiotics crisis, the use of antimicrobial-loaded liposomes as delivery vehicles shows great promise. This innovative approach not only extends drug effectiveness and reduces toxicity but also provides a path to address highly resistant infectious conditions. As research advances, liposomal nanotherapeutics may emerge as a transformative solution in the fight against bacterial infections.
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Cancer has been an enormous pain point for patients and regulatory bodies across the globe. In Dec. 2023, the US FDA released guidance on benzene-grade carbomer formulations, which triggered pharmaceutical manufacturers to assess risk, test finished products, and reformulate drug products with benzene-grade carbomer. The immediate implementation of the stoppage of finished products with benzene-grade carbomers has threatened pharmaceutical excipients and finished product manufacturers. The gravity of this situation prompted the US Pharmacopeia to extend the deadline for discontinuation from August 1, 2025, to August 1, 2026, allowing manufacturers ample time for reformulation and regulatory compliance. There is an immediate need to understand the guidance and to learn how manufacturers should do the risk assessment and approach reformulation. This review provides an in-depth analysis of the risk assessment and reformulation processes involved in various dosage forms utilizing benzene-grade carbomer, supported by specific case studies. This review offers insights into navigating the USFDA guidelines to ensure formulation safety and compliance, thus enabling pharmaceutical practitioners to uphold the highest standards of patient care and tackle life cycle management challenges. The decision of the USFDA to restrict the usage of high benzene content of carbomer in the formulation is a welcome move. This article has shown a way for researchers to see opportunities in the path and provide best-in-class medicines to patients with a better formulation safety profile.
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This book series invites all the Specialists, Professors, Doctors, Scientists, Academicians, Healthcare professionals, Nurses, Students, Researchers, Business Delegates, and Industrialists across the globe to publish their insights and convey recent developments in the field of Nursing, Pharmaceutical Research and Innovations in Pharma Industry. Book series on Pharmacy and Nursing covers research work in a set of clinical sciences and medicine.
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When contrasted with conventional skin arrangements, film-framing showers can give steady medicine dispersion and portion, improved bioavailability, decreased aggravation, nonstop medication delivery, and fast twisted recuperating through dampness control. Polymers and excipients in film-shaping showers work on the properties of arrangements and increment the soundness of dynamic substances. Every polymer and excipient will yield films with unmistakable attributes. In order to improve a film-forming spray, various polymers and excipients, as well as their assessment criteria, must be investigated. The writing survey covered examinations on polymers as film-shaping grids and the utilization of these showers for restorative purposes or expected clinical applications. This article discusses the essential criteria for determining spray ability and film properties, as well as the types and concentrations of polymers and excipients, sprayer types, evaluations, and other factors. According to the review, topical medication administration can be improved by using either naturally occurring or man-made polymers that have viscoelastic or in situ film properties. Introduction to FFS [1-20] Skin courses of medication conveyance go for the gold neighborhood impacts and proposition different benefits, including keeping away from first-pass digestion and the impact of low pH and catalysts in the gastrointestinal plot, as well as an enormous accessible surface area. To work on restorative efficiency or pharmacokinetic profiles, drugs managed through the skin course are for the most part made in a measurement framework, like a fix, gel, moisturizer, cream, treatment, or spray. Nonetheless, the worry is that fix arrangements actually leave drug deposits after use and can be purposely abused. Fix arrangements are additionally frequently connected with excessive touchiness, disturbance, and blistering. Issues in the scale-up of creation are additionally frequently found where medications are difficult to balance out and can take shape during storage. Other semisolid arrangements likewise have the drawback of being handily joined to dress while moving and can cause cross-contamination of wounds since it is applied utilizing the fingers. Contrasted with other skin dosages,sprays offer a few benefits, for example, reasonable use, low rate of bothering, sterility of the dose, brilliant inclusion of the skin or twisted, even dispersion of the medication when applied, and flexible dosage. In late many years, different advancements have kept on being created to acquire efficient and viable shower arrangements. One of them is a film-shaping shower (FFS) which has been applied in numerous fields, like the food business, beauty care products, drugs, manors, etc. FFS for the most part comprises of dynamic substances, enhancers, and polymers that are broken up in natural solvents. A flimsy, non-tacky film structures that can expand the contact time and porousness of the medication, bringing about ceaseless medication discharge, and can forestall crys-tallisation so that more medication is accessible to give therapeutic impacts contrasted with other ordinary skin arrangements.
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Neurological disorders such as Alzheimer’s disease, Parkinson’s disease, epilepsy, glioma, depression, and anxiety are seriously affecting humans across the globe. Currently, FDA-approved medicines are practiced using conventional drug delivery systems to treat these brain disorders. Moreover, these delivery systems fail to provide sufficient drug concentration in the brain to achieve therapeutic efficacy due to the presence of a blood–brain barrier. Hence, researchers explore nanoparticle-based delivery systems with different administration routes such as oral, parenteral, or intranasal to treat brain disorders. Among the different routes, the intranasal or nose-to-brain drug delivery approach is frequently explored recently to target the brain. In this context, the nose-to-brain delivery approach with nanoparticle-based systems such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, mesoporous silica nanoparticles, nanoemulsions, and polymeric nanoparticles has been majorly explored to treat the neurological disorders. However, different factors critically affect efficient drug delivery via the nasal cavity in treating neurological disorders. Thus, this book chapter briefly discusses the factors and challenges associated with nose-to-brain delivery. In addition, important formulation aspects such as particle size, shape, surface charge, surface modification, and pH are critically evaluated for better delivery of drugs to the brain. Further, the key potential of the nose-to-brain approach using different nanoparticles in treating neurological disorders is briefly highlighted in this compilation.
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Topical drug delivery is widely used in various diseases because of the advantages of not passing through the gastrointestinal tract, avoiding gastrointestinal irritation and hepatic first-pass effect, and reaching the lesion directly to reduce unnecessary adverse reactions. The skin helps the organism to defend itself against a huge majority of external aggressions and is one of the most important lines of defense of the body. However, the skin’s strong barrier ability is also a huge obstacle to the effectiveness of topical medications. Allowing the bioactive, composition in a drug to pass through the stratum corneum barrier as needed to reach the target site is the most essential need for the bioactive, composition to exert its therapeutic effect. The state of the skin barrier, the choice of delivery system for the bioactive, composition, and individualized disease detection and dosing planning influence the effectiveness of topical medications. Nowadays, enhancing transdermal absorption of topically applied drugs is the hottest research area. However, enhancing transdermal absorption of drugs is not the first choice to improve the effectiveness of all drugs. Excessive transdermal absorption enhances topical drug accumulation at non-target sites and the occurrence of adverse reactions. This paper introduces topical drug delivery strategies to improve drug effectiveness from three perspectives: skin barrier, drug delivery system and individualized drug delivery, describes the current status and shortcomings of topical drug research, and provides new directions and ideas for topical drug research.
Experiment Findings
This study investigates and compares locally developed starches derived from three different grains: Ilaje rice, Igbimo rice, and Efon-alaye rice. These grains are rich in carbohydrates, but their starch composition varies, which affects their suitability as pharmaceutical excipients. The starch powders were analyzed for chemical composition (protein, ash, fat, crude fiber, and amylose content) and characterized for particle size and distribution using scanning electron microscopy (SEM). Physicochemical properties such as pH, viscosity, hydration capacity, swelling capacity, moisture sorption capacity, bulk density, tapped density, Carr's Index, and Hausner's ratio were evaluated. The starch powders successfully passed identification and solubility tests according to the BP (British Pharmacopoeia) guidelines. Igbimo rice starch exhibited the lowest Carr's Index, Hausner's ratio, and moisture sorption capacity while demonstrating the highest hydration and swelling capacity among the three starches. Consequently, Igbimo rice starch demonstrated the best flowability and compressibility properties among the three starches. These findings contribute to the knowledge of starch properties and support the exploration of locally sourced rice starch as potential tablet excipients in pharmaceutical applications.
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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.
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The review focuses on the lipid based nanocarriers, with special attention paid to natural bioactive payloads. First, micelles and microemulsions are considered as very attractive colloidal nanocontainers that allow for marked improving the solubility of hydrophobic bioactives. Further, liposomal vehicles are reviewed, with both advantages and limitations discussed. Literature assay covers up-to-date information of about last three to five years, although brief background is given on the pioneer works addressing the liposomes and their evolution from bench to bedside. Final part of the review is devoted to the modern modifications of vesicular nanocarriers which can be adapted to specific administration way due to improved targeting properties, permeability, mucoadhesiveness and possibility to cross biological barriers. Therein, such kinds of nanocarriers as transfersomes, niosomes, ethosomes, chitosomes are evaluated; and separate sections focus on the natural based formulations, i.e., phytosomes and invasomes.
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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.
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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.
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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.
Chapter
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
Chapter
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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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