Formulation Development, In Vitro and In Vivo Evaluation of Topical Hydrogel Formulation of Econazole Nitrate-Loaded β-Cyclodextrin Nanosponges

益康唑 环糊精 Box-Behnken设计 化学 体内 渗透 色谱法 药理学 响应面法 抗真菌 皮肤病科 医学 生物化学 生物技术 生物 咪康唑
作者
Shivansh Srivastava,Alok Mahor,Gyanendra Singh,Kuldeep K. Bansal,Prem Prakash Singh,Rishikesh Gupta,Rohit Dutt,Amer M. Alanazi,Azmat Ali Khan,Prashant Kesharwani
出处
期刊:Journal of Pharmaceutical Sciences [Elsevier]
卷期号:110 (11): 3702-3714 被引量:26
标识
DOI:10.1016/j.xphs.2021.07.008
摘要

Econazole nitrate, an antifungal drug used in the handling of skin ailments, is commercially not efficient as these ailments typically require a more elevated concentration of the drug to offer an effective pharmacological retort. Like so, it is proposed to assess the effectiveness of the topical hydrogel of econazole-loaded nanosponge in the management of skin ailment(s). Econazole nitrate-laden β-cyclodextrin nanosponges were developed by employing the melt method using β-cyclodextrin as the organic polymer and N,N-carbonyldiimidazole as the crosslinker. The critical factors disturbing the quality of the formulation were uniquely identified by the Ishikawa diagram, and they were optimized by the statistical experiment design concept. β-cyclodextrin loaded nanosponges were uniquely designed using the Placket-Burman approach and optimized utilizing the Box-Behnken method. The optimized nanosponges (EN-CDN) were 421.37 ± 6.19 nm in size with an entrapment efficiency of 70.13% ± 5.73%. The topical hydrogel of nanosponges (EN-TG) was prepared using carbopol 934 and pyrrolidone as permeation enhancers. In vitro skin permeation studies affirmed the improved transport crosswise the goatskin for topical hydrogel in comparison to the marketed product. EN-TG was able to control the fungal infection in the selected animal model in comparison to the marketed preparation. Stability studies reported favorably that nanogel remained stable under normal and accelerated settings.
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