Background:The purpose of this study was to develop microemulsion-based hydrogel formulation for topical delivery of bifonazole with an objective to increase the solubility and skin permeability of the drug.Materials and Methods:Oleic acid was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems. The pseudo-ternary phase diagrams for microemulsion regions were constructed using oleic acid as the oil, Tween 80 as the surfactant and isopropyl alcohol (IPA) as the cosurfactant. Various microemulsion formulations were prepared and optimized by 32 factorial design on the basis of percentage (%) transmittance, globule size, zeta potential, drug release, and skin permeability. The abilities of various microemulsions to deliver bifonazole through the skin were evaluated ex vivo using Franz diffusion cells fitted with rat skins. The Hydroxy Propyl Methyl Cellulose (HPMC) K100 M as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The optimized microemulsion-based hydrogel was evaluated for viscosity, spreadability, skin irritancy, skin permeability, stability, and antifungal activity by comparing it with marketed bifonazole cream.Results:The mechanism of drug release from microemulsion-based hydrogel was observed to follow zero order kinetics. The studied optimized microemulsion-based hydrogel showed a good stability over the period of 3 months. Average globule size of optimized microemulsion (F5) was found to be 18.98 nm, zeta potential was found to be -5.56 mv, and permeability of drug from microemulsion within 8 h was observed 84%. The antifungal activity of microemulsion-based hydrogel was found to be comparable with marketed cream.Conclusion:The results indicate that the studied microemulsion-based hydrogel (F5) has a potential for sustained action of drug release and it may act as promising vehicle for topical delivery of ibuprofen.
Ageing is the phase of gradual decline of body efficiency and metabolic activities after reaching a maturity stage. Free radicals cause oxidative alterations in collagen, elastin material and changes in membrane characteristics and induce polymerization reactions. Use of topical antioxidants can overcome some of these effects and retard actinic ageing. Herbal products are popular due to their minimum risk of side-effects with maximum efficacy. The present study was undertaken to evaluate the antiageing potential of Benincasa hispida fruit extract as not many scientific studies have been carried out to explore its utility as skin renewal enhancer and as an antioxidant. After removing the outer layer and the seeds, the fruit pulp was dried. The dried fruit pulp was extracted successively with petroleum ether, chloroform, ethyl acetate and methanol by Soxhlation for 2 days. Methanol was recovered under vacuum and a dry extract was obtained (yield 4.2% w/w), which was stored in a desiccator. Suitable topical cream base for effective carriage of fruit extract was developed and its in vitro evaluation for skin renewal activity was tested by application to the stratum corneum of human cadaver skin and by dansyl chloride fluorescence method. The results show that the cream prepared from Benincasa fruit extract may prove as an antiageing preparation and can be used for retarding the symptoms of ageing.
Objective: To develop bioadhesive ocular inserts of Olopatadine hydrochloride for treating the allergic eye conditions with sustained ocular delivery which will reduce dosing frequency. Methods: Matrix type ocular inserts were prepared by the solvent casting technique using teflon coated petri plates and characterized in vitro for drug release studies. Nine formulations were prepared having different ratios of polymers such as carbopol 980P, HPMC K4M and NaCMC (90:10, 70:30 and 50:50) and optimized. All the formulations were evaluated for thickness, weight variation, folding endurance, drug content uniformity, in vitro release study, bio/mucoadhesion studies, surface pH, swelling index, % moisture absorption, % moisture loss, release kinetics, histological study and stability study. Results: The optimized formulation 'F5' containing polymers Carbopol 980P and HPMC K4M in the ratio of 70:30 was selected on the basis of drug release studies. The formulation F5 was found to act as bio/mucoadhesive insert with sustained drug release by increasing residence time in the eye. Conclusion: The prepared inserts showed sustained drug release by increased residence time achieved through bioadhesion and thus may overcome the drawbacks of eye drops.
Background:The purpose of the present research work was to extract jackfruit mucilage, use it as a mucoadhesive agent, and to develop extended release buccoadhesive tablets with an intention to avoid hepatic first-pass metabolism, by enhancing residence time in the buccal cavity.Materials and Methods:The mucilage was isolated from the jackfruit pulp by the aqueous extraction method and characterized for various physiochemical parameters as well as for its adhesive properties. Three batches of tablets were prepared (wet granulation method) and evaluated containing three mucoadhesive components: Methocel K4M, Carbopol 974P, and isolated jackfruit mucilage using chlorpheniramine maleate (CPM) as a model drug and changing the proportion of the mucoadhesive component (1:2:3), resulting in nine different formulations.Results:The results of the study indicate that the isolated mucilage had good physicochemical and morphological characteristics, granules and tablets conformed to the Pharmacopoeial specifications, and in vitro release studies showed the sustained action of drug with increasing concentration of the isolated natural mucoadhesive agent in the formulations. Permeability studies indicated that changing the mucoadhesive component, permeability behavior was not statistically different (P > 0.05). FTIR and UV spectroscopy studies between mucilage and CPM suggested the absence of a chemical interaction between CPM and jackfruit mucilage.Conclusion:The developed mucoadhesive tablets for buccal administration containing natural mucilage (MF3) have a potential for the sustained action of drug release. Thus, mucoadhesive tablets for controlled release were successfully developed using natural jackfruit mucilage.
Waxes have been used in many cosmetic preparations and pharmaceuticals as formulation aids. Rice bran wax is a byproduct of rice bran oil industry. Present study aims to investigate possible use of rice bran wax as occlusive moisturizer. The rice bran wax obtained was purified and its physicochemical characteristics were determined. In vitro studies were carried out to determine trans epidermal water loss through stratum corneum and water holding capacity of stratum corneum of human cadaver skin treated with pure rice bran wax and formulation of rice bran wax. The results show that rice bran wax can be used as a promising occlusive moisturizer.
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