Formulation and Evaluation of Clotrimazole Niosomal Gel for Topical Application

S. Shirsand, G. Kumar, G. Keshavshetti, S. Sharanabasappa, P. V. Swamy
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引用次数: 10

Abstract

Objective: In the present investigation, an attempt is made to develop and characterize niosomal gel formulation of clotrimazole to increase retention time in the dermis layer through controlled release of the drug. Methodology: Clotrimazole niosomes were prepared by thin film hydration method using span 40 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). The niosomal dispersion was evaluated for vesicle size, surface morphology, percent entrapment efficiency and in vitro drug release. Results: Among the five formulations prepared, the formulation CN3 (containing 100 mg drug, 200 mg surfactant) was found to be promising. Selected niosomal suspension (CN3) containing clotrimazole equivalent to 2 % w/w was incorporated into gel base composed of carbopol (1%), triethanolamine 0.3% and distilled water quantity sufficient. The gel was studied for it’s different parameters such as pH, in vitro drug release, anti-fungal activity and skin irritation effect. Conclusion: The studies suggest that encapsulating clotrimazole in nonionic surfactant vesicles would provide better patient compliance by achieving prolonged release of the drug to the dermis with improved efficacy.
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外用克霉唑乳质体凝胶的研制及评价
目的:研制并表征克霉唑乳质体凝胶制剂,通过控释增加药物在真皮层的滞留时间。方法:以span 40(非离子表面活性剂)和胆固醇(稳定囊泡形成剂)为原料,采用薄膜水合法制备克霉唑乳小体。用囊泡大小、表面形态、包封率和体外药物释放率等指标评价膜体分散度。结果:制备的5个制剂中,CN3(含药物100 mg,表面活性剂200 mg)的前景较好。选择含有相当于2% w/w的克霉唑(clotrimazole)的niosomal suspension (CN3),加入到carpool(1%),三乙醇胺0.3%,蒸馏水量足够的凝胶基中。研究了该凝胶的pH、体外药物释放、抗真菌活性和皮肤刺激效果等参数。结论:研究表明,在非离子表面活性剂囊泡中包封克霉唑可以延长药物向真皮的释放时间,提高疗效,从而提高患者的依从性。
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