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Investigation of biological membrane permeability of nanoemulsion, nanostructured lipid carriers and lipid polymer hybrid nanocarriers based nanogel as transdermal carvedilol delivery system
Abstract
Carvedilol was antihypertensive and antioxidant properties. It was practically water insoluble. It undergoes extensive hepatic first pass metabolism. The aim of this research to study permeability coefficient for NE, NLCs and LPHNs based nanogel through biological membrane using carvedilol as transdermal drug delivery system (TDDS). Aqueous phase titration, ultrasonic emulsion evaporation and microwave-based methods were used to prepare NE1-NE3, NLC1-NLC3 and LPHN1-LPHN3 respectively then subject to various measurements. The formulated lipid-based nanoparticles NE1-LPHN3 were employed as base to prepare lipid base nanogel G1-G9 that was compare to already prepared conventional gel of carvedilol (G). It was found colloidal features associated with the carvedilol loaded lipid-based nanoparticles NE1-LPHN3. The biomembrane permeation evaluation of G1-G9 formulations was indicated that the permeability coefficient (cm/min) of drug was significantly higher (p-value <0.05) for G1 and was significantly lower (p-value < 0.05) for conventional carvedilol gel (G). The preparation and evaluation processes were emphasized that G1-G9 suitable to deliver across biomembrane. The drug that was contained in LPHN based nanoglobules had lower ability to pass through experimental skin that gave it more ability to control drug diffusion in comparison to NE and NLCs.
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Purpose: Felodipine, is a calcium-channel antagonist used for hypertension and angina pectoris. It is practically insoluble in aqueous media and shows low oral bioavailability (15%-20%). This investigation aims to prepare and characterize oral felodipine lipid-polymer hybrid nanocarriers (LPHNs) to increase solubility and control delivery for increasing bioavailability and enhance patient compliance.
Methods: The newly microwave-based method was prepared with felodipine LPHNs (H1-H35) successfully. The (H1-H35) were subjected to thermodynamic stability experiments. After that, select nine felodipine LPHNs (F1-F9) that have smart physical stability for further optimization of different characterization processes.
Results: The felodipine LPHNs (F4) are considered the most optimized formula. It was characterized by lower particle size (33.3 nm), lower PDI (0.314), high zeta potential (13.6 mV), entrapment efficiency is (81.645% w/w), drug loading is (16.329% w/w), the pH value is 4, excellent percent of light transmittance (95.5%), pseudoplastic rheogram, significantly high (P < 0.05) dissolution rate with sustained drug delivery and success ex-vivo intestinal permeation attributes. The (F4) subject for further investigations of Fourier transformed infrared spectroscopy (FTIR), atomic force microscopy (AFM), and transmission electron microscopy (TEM). The results of FTIR, AFM, and TEM indicate there is no interaction between the felodipine and excipients and that the particulate system in the nanoscale dispersion system confirms the high stability.
Conclusion: The optimized felodipine LPHNs (F1-F9) formulations were smart formulations for sustained oral delivery of felodipine and that F4 was the most optimized formula according to its characterization processes.
Nanotechnology recently emerged among the most exciting science-related innovations. Nanotechnology-produced metal nanoparticles got a lot of attention. This is emerging as a rapidly developing field due to its effective applications that targeted the manufacturing of new materials at the nanoscale level. There is considerable interest in the application of nanomaterials in many areas of industry including agrifood and biomedical products. In the agrifood area, nanomaterials have benefits in diverse areas which include fertilizers, herbicides, pesticides, sensors, and quality stimulants, among other food processing, food packaging, and nutraceuticals to improve nutritional value. These applications in agriculture result in enhanced quality and crop yield, reduction in pollution caused by various chemicals, etc. In the pharmaceutical area, nanomaterials are claimed to ameliorate drug safety and efficacy, as well as bioavailability. They are utilized for targeting various drugs to a specific location in the body. However, there are also concerns that some nanoparticles may have adverse effects on human health. These include titanium dioxide, copper oxides, and other nanomaterials which lead to liver damage, skin damage, lung damage, and various other human health-related problems. This review is aimed at presenting a briefing on the state of the art in the application of nanotechnology in food and human nutrition and drug administration, consumer attitudes, and their challenges and opportunities with future perspectives.
Various non-invasive administrations have recently emerged as an alternative to conventional needle injections. A transdermal drug delivery system (TDDS) represents the most attractive method among these because of its low rejection rate, excellent ease of administration, and superb convenience and persistence among patients. TDDS could be applicable in not only pharmaceuticals but also in the skin care industry, including cosmetics. Because this method mainly involves local administration, it can prevent local buildup in drug concentration and nonspecific delivery to tissues not targeted by the drug. However, the physicochemical properties of the skin translate to multiple obstacles and restrictions in transdermal delivery, with numerous investigations conducted to overcome these bottlenecks. In this review, we describe the different types of available TDDS methods, along with a critical discussion of the specific advantages and disadvantages, characterization methods, and potential of each method. Progress in research on these alternative methods has established the high efficiency inherent to TDDS, which is expected to find applications in a wide range of fields.
The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of 92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal permeation study using the non-everted sac model shows four folds increment in the permeation of DE-NLCs compared to dabigatran etexilate suspension (DE-S).
Objective: The main objective of this experiment was to prepare and optimized celecoxib nanoemulgel. This formulation can be used for acuterheumatoid arthritis patients.Methods: Celecoxib is a poorly water soluble drug. We prepared celecoxib nanoemulgel to improve intrinsic solubility of celecoxib and enhancedeeper permeation throughout the skin. After several screening, the combination of acetonitrile, triacetin, campul 908P was considered for oil phase;acconon MC8-2EP as surfactant, and capmul MCM C-10 as a co-surfactant accordingly. As per Box-Behnken surface design model, optimization wasdone for all the 13 formulations.Results: Based on pseudo ternary plot, it was found that 4:1 Smix ratio was optimum and possessed maximum drug solubility. Further, screeningshown, 0.25-0.75% carbopol-940 can be a stable candidate for hydrogel preparation. Prepared nanoemulsions and hydrogels were admixed to preparenanoemulgel. Based on overlay plot, EG14* formulation was consider as optimum one, and various evaluation parameters were performed along withother formulations. Using Franz diffusion cell, in-vitro diffusion studies was performed. Almost all the formulations produces good qualitative drugrelease profile. The EG14* shown 95.50% drug release after 12th hrs with standard Higuchi plot (R2 value 0.9989). The optimum viscosity was foundto be 521±0.81 mPas at 100 rpm. The appearance of the formulations was milky, yellowish white with expectable pH ranged from 5.8 to 6.7. Theoptimized formulation has good spreadability coefficient, good ex-vivo diffusion enhancement factor (3.03) as compare to marketed gel. Mostly, ourformulations have less skin irritation and higher anti-inflammatory activity (92.56% of inhibition of paw edema for EG14*).Conclusion: From the thermodynamic studies, it was confirmed that EG14* maintained excellent stability profile in various heating-cooling cycle,centrifugation, and freeze-thaw cycle condition. Hence, it can be conclude that, our formulation, can be consider for pilot scale up.
Nanostructured lipid carriers (NLCs) are modified solid lipid nanoparticles (SLNs) that retain the characteristics of the SLN, improve drug stability and loading capacity, and prevent drug leakage. Polymer nanoparticles (PNPs) are an important component of drug delivery. These nanoparticles can effectively direct drug delivery to specific targets and improve drug stability and controlled drug release. Lipid-polymer nanoparticles (PLNs), a new type of carrier that combines liposomes and polymers, have been employed in recent years. These nanoparticles possess the complementary advantages of PNPs and liposomes. A PLN is composed of a core-shell structure, the polymer core provides a stable structure, and the phospholipid shell offers good biocompatibility. As such, the two components increase the drug encapsulation efficiency rate, facilitate surface modification, and prevent leakage of water-soluble drugs. Hence, we have reviewed the current state of development for the NLCs’, PNPs’, and PLNs’ structures, preparation, and applications over the past five years, to provide the basis for further study on a controlled release drug delivery system.
The present objective for the study was to prepare proliposomal gel bearing a steroidal anti-inflammatory agent, prednisolone intended for topical application. Various proliposome formulations were prepared using thin film hydration technique by varying the lipid phase composition (lecithin/cholesterol). Proliposome formulations were characterized for drug content, entrapment efficiency, surface morphology, surface charge, FTIR and stability studies. Topical proliposomal gels were prepared by incorporation of proliposome into strusctured vehicle carbopol (2%). Alternatively, hydrogels containing prednisolone were prepared and their drug release properties were investigated. Pharmacodynamic activity was also determined for optimized proliposomal gel and was compared with commercial marketed gel. A spherical shape of reconstituted prednisolone liposome with an average vesicle about 2~6μm was observed in photomicrographs. The percentage entrapment of drug was increased with increase in phospholipid composition in the range of 85-98%. FTIR studies showed no possible drug-excipient interaction. Proliposomal gel showed prolonged release of prednisolone than the hydrogels. Anti-inflammatory activity proliposomal gel showed maximum percentage of inhibition of edema 60% when compared to commercial marketed gel 55%. Stability studies indicated that product is stable and should be stored at low temperatures. Proposed prednisolone proliposomal gel showed sustains release with enhanced anti inflammatory activity implicating its potential in effective topical pharmacotherapy for the treatment of rheumatoid arthritis.
Basically Emulsions are liquid–liquid dispersions along with one liquid phase which is dispersed in the other liquid phase as small sized droplets. These days, there is an increasing interest in the utilization of nano emulsions in pharmaceuticals as well as cosmetics industry because of it’ snumerous of potential advantages over conventional and microemulsions. Nanoemulsions are nano-sized emulsions which have sizes range from tens to hundreds of nano meters. Nano emulsion sex hibit useful characteristics due to its small droplet size which leads to high surface area per unit volume, higher stability, optically transparent appearance, flexible fluidity as well as increased bioavailability of lipophilic components. The current review provides a comprehensive overview, starting with an introduction of nano emulsion types, preparation methods, stability study, characterisation, and applications of nano emulsion.
Objective: The objective of current study was to formulate and characterize nanolipid carriers of paclitaxel with increased solubility and % release profile of the drug which leads improvement of bioavailability. Methods: It is proposed to incorporate the hydrophobic anticancer drug such as paclitaxel in NLCs to increase the bioavailability and solubility of the therapeutic agent and to assess the developed formulation’s efficacy by in-vitro drug release profile. The main intents of the study are to utilize the various attributes of the proposed biopolymer (glycerol caprate) for the preparation of NLCs to encapsulate paclitaxel. The objectives of the study are to appraise the morphological, physiochemical characteristics of the developed system with their in-vitro performance. Result: The result of the NLCs characterization was evaluated by Zeta potential, poly dispersity index (PDI), percentage entrapment efficiency, drug loading, solubility and partition co-efficient. Conclusion: The result concluded stable NLCs formulation with improved solubility and extended in-vitro drug release.
This study was aimed at the development of natamycin loaded nano-structured lipid carriers (NLCs) and their characterization for physicochemical properties i.e., Fourier Transform Infrared (FTIR), UV-Visible spectroscopy, meting point, solubility profile and partition coefficient. FTIR and Differential Scanning Calorimetry (DSC) permit the characterization of the drug, excipients and binary mixture and thus assisted in predicting the compatibility of natamycin with other excipients. Lipid screening for formulation of NLCs were performed by their solubility and drug affinity studies. High homogenization and sonication method was employed for the development of natamycin loaded NLCs and it was characterized for vesicle size, zeta potential, % entrapment efficiency, viscosity, pH and percentage drug release up to 12 h.
Objective: The purpose of this study was to develop salmeterol, fluticasone nano-lipid carriers to estimate as potentials of oral delivery system for poorly water soluble drugs. Nano-lipid carriers applied to chronomodulated pulsatile drug delivery system maintain the concentration level by releasing the drug at predetermined time interval throughout the management of asthma. Method: The particle size analysis revealed that all the formulations were within the nanometer range of 150.0±2.4nm. Percentage of entrapment efficiency and drug loading were found to be 69.5±4.4 - 85.3±1.3 and 9.358±2.2-10.45±8.1, respectively. The SLM-FCN nano-lipid carrier’s optimized formulation showed spherical morphology with smooth surface under the transmission electron microscope (TEM), the crystalline characterization of drug in NLC was investigated by X-ray diffraction and differential scanning calorimetric (DSC). The ex-vivo permeation study showed many folds increment in the SLM-FCN NLCs compared to powder SLM-FCN 96.0±2.55 and pulsing plugs in-vivo drug released effectively in pre-determine time intervals. Conclusion: The progression concludes that chronomodulated programming pulsatile release was achieved with modified pulsing bilayerd plugged of salmeterol, fluticasone propionate NLCs, formulation remarkably improved oral bioavailability. we promise that finding in this investigations suggest practicability of the dosage form system can be taken after at bedtime then it will be delivered in the early morning which maintains the drug concentration throughout to control asthma.
The aim of the present study was to develop a Cisplatin loaded NLCS to enhanced and effective delivery of drug to the skin cancer. NLCS bearing Cisplatin were prepared by emulsification solvent diffusion method. The formulated NLCS were characterised for average particle size, polydispersity index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations were studied for its in vitro cell line and cell uptake study. It was revealed that the average size of NLCS was found 172.2±3.2, PDI was 0.135, % entrapment efficiency was found 68.9±2.04 and Zeta potential was found-15.3±1.3. In-vitro release determined by Frenz diffusion cell was found 63.7±2.8% after 72 hr. MTT assay shows that Cisplatin loaded NLCS were giving more cytotoxity as compare to plain drug. The cell uptake study was found enhanced uptake of FITC loaded NLCS in comparison to plain FITC. Cisplatin and Cisplatin loaded NLCS showed 22.3±1.2 and 32.8±0.9 growth inhibition respectively after 48h upon incubation at 0.5 µg/mL concentration (p<0.05). The result of the studies was concluded that NLCS can be use as impending drug delivery system which may enhance the drug uptake and maintain the drug level for longer period of time and it is potential carrier system which can be use for the treatment of skin diseases like cancer.
This review article is an updated overview on lipid-polymer hybrid nanoparticles (LPHNs) including the various types of LPHNs polymers used in their preparation, various methods of preparation, their physiochemical, in-vitro and in-vivo evaluation parameters and their application in various delivery systems. LPHNs show a combined advantage of biodegradable polymeric nanoparticles and liposomes. LPHNs mainly consist of a biodegradable polymeric material core containing drugs or any substances which are to be encapsulated then this core is further enclosed by a phospholipid layer i.e. lipid PEG layer. LPHNs show good physical strength and biocompatibility. The hybrid structural design can offer various benefits such as controlled particle size, high drug loading, surface functionality with various ligands (antibody fragments, peptides, monoclonal antibodies, aptamers, and folate molecules), and encapsulation of combinational therapeutic agents, showing prolonged release of drug and drug circulates in the blood for longer duration. Significantly, the LPHNs have recently been confirmed as a better drug delivery route and good cellular delivery efficacy of various drugs as compared to polymeric nanoparticles and liposomes.
Nanoemulsions are transparent system mostly covering droplet size in nanometric scale because of their small droplet sizes. Nanoemulsion appears transparent and is kinetically stable. The long term physical stability of nanoemulsion makes them unique and is sometime referred as ‘Approaching Thermodynamic stability’. These increases the rate of absorption eliminates variability in absorption and increase bioavailability. These can carry lipophilic and hydrophilic drugs. This review aims on the method of preparation, characterization techniques, advantages and disadvantages and the various route of drug delivery of nanoemulsion.
Objective: Carvedilol is antihypertensive. It is practically water insoluble. Therefore, the objective of this investigation is a formulation and characterization of carvedilol nano emulsion (NE) employing orally to increase carvedilol solubility for enhancing of carvedilol bioavailability. Methods: The formulation components were chosen according to the solubility study. The diagrams of pseudo-ternary phase were made using the aqueous phase titration method. The formulated nanoemulsions were subjected to various thermodynamic stability assays. We selected eight of formulas that have thermodynamic stability for further optimization for various characterizations in order to select the best formula. Results: The carvedilol NE3 considered a selected formula. It composes of 1.25 mg carvedilol per g of the nanoemulsion, 10% of peppermint oil, 20% of tween80, 10% ethanol and 60% of distilled water. It was characterized by a low globule size range, low poly dispersity index, higher zeta potential, good pH value, efficient electroconductivity, classy percent of light transmittance, higher % drug content, acceptable low viscosity and carvedilol release was significantly higher (P<0.05) in dissolution rate. The carvedilol NE3 subject for further investigations. Fourier transformed infrared spectroscopy confirm no incompatibility between the drug and excipients. The atomic force microscopy study shows that system in nanoscale and has high stability. Conclusion: The selected formula (carvedilol NE3) was a promising nanoemulsion formula that increases the carvedilol solubility result in an increment of its bioavailability. © 2015, International Journal of Pharmacy and Pharmaceutical Science. All rights reserved.
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