天然油纳米乳液凝胶载体增强鲁立唑局部抗菌作用

Ahmed M. Kmkm, Mowafaq M. Ghareeb
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引用次数: 1

摘要

背景:鲁立康唑是一类新型咪唑类抗真菌剂,对多种真菌,尤其是皮肤癣菌有很好的防治效果。它具有非常低的水溶性,作为局部递送的屏障,并限制了其皮肤可用性。研究目的:采用水滴定法制备鲁立唑油/水纳米乳液。方法:通过溶解度研究,选择薄荷油、吐温80和transcutol p分别作为油相、表面活性剂和助表面活性剂,尽管假三元相图构建了用于筛选配方的纳米乳液区域。制备了15种o/w纳米乳液配方,并对其液滴大小、多分散指数、pH值、透光率百分比、鲁立唑含量进行了表征。在配方中,引入了八种制剂,通过结合0.5%卡波姆934作为胶凝剂来提高所制备的纳米乳液的粘度。结果:所选制剂显示出均匀的纳米乳液,其pH值适合皮肤应用,并可接受鲁立唑的含量。粘度结果表明,具有剪切稀化粘度分布的非牛顿拟塑性行为。体外释放研究显示,与纯鲁立康唑分散体相比,释放曲线(f2 50)不同。结果表明,油∶Smix(2:1)∶水(15:40:43.5)比例为1%药物和0.5%卡波姆934的配方NG-1是具有优异铺展性的优化配方。结论:该研究得出的结论是,基于纳米乳液的凝胶有望成为一种令人鼓舞的、持续不断的技术,用于局部制备并提高水溶性药物在皮肤上的溶解度、溶解速率和渗透性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Natural Oil Nanoemulsion-Based Gel Vehicle for Enhancing Antifungal Effect of Topical Luliconazole
Background: Luliconazole, a newer class of imidazole anti-fungal agent, is very effective against several species of fungi, especially dermatophytes. It has very low aqueous solubility acting as barrier for topical delivery and limiting its dermal availability. Aim of the study: This study aimed to formulate luliconazole oil/water nanoemulsion by the aqueous titration method. Methods: Solubility study resulted in selecting peppermint oil, tween 80 and transcutol p as oil phase, surfactant and cosurfactant respectively, although pseudoternary phase diagram construct nanoemulsion area for picking formulations. Fifteen o/w nanoemulsion formulations prepared and characterised for droplet size, polydispersity index, pH values, percent transmittance, luliconazole content. Among formulations, eight preparations introduced to enhance the viscosity of prepared nanoemulsion by combining 0.5% carbopol 934 as gelling agent. Results: The selected preparations demonstrated homogeneous nanoemulgels with pH values appropriate for skin application and accepted luliconazole content. Viscosity results manifested non-newtonian pseudo plastic behavior with shear-thinning viscosity profile. In vitro release studies revealed dissimilar release profile (f2˂50) than that of pure luliconazole dispersion. The results revealed that the formula NG-1 with oil: Smix(2:1):water (15:40:43.5) ratio containing 1% drug and 0.5% carbopol 934 was the optimised formula with excellent spreadability. Conclusion: The study concluded that nanoemulsion-based gel is contemplated an encouraging and proceed technique for the topical preparation and upgrade solubility, dissolution rate and permeability of insufficient water-soluble drugs across the skin.
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