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硝酸益康唑的黏膜黏附水凝胶薄膜：采用析因设计的处方与优化

Mucoadhesive hydrogel films of econazole nitrate: formulation and optimization using factorial design.

作者信息

Gajra Balaram, Pandya Saurabh S, Singh Sanjay, Rabari Haribhai A

机构信息

Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT Campus, Changa, Petlad Taluka, Anand District, Gujarat State 388421, India.

Shree Krishna Institute of Pharmacy, Krishna Campus, Shankhalpur, Bechraji Taluka, Mehsana District, Gujarat State 384210, India.

出版信息

J Drug Deliv. 2014;2014:305863. doi: 10.1155/2014/305863. Epub 2014 Jun 10.

DOI:10.1155/2014/305863
PMID:25006462
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4071986/
Abstract

The mucoadhesive hydrogel film was prepared and optimized for the purpose of local drug delivery to oral cavity for the treatment of oral Candidiasis. The mucoadhesive hydrogel film was prepared with the poly(vinyl alcohol) by freeze/thaw crosslinking technique. 3(2) full factorial design was employed to optimize the formulation. Number of freeze/thaw cycles (4, 6, and 8 cycles) and the concentration of the poly(vinyl alcohol) (10, 15, and 20%) were used as the independent variables whereas time required for 50% drug release, cumulative percent of drug release at 8th hour, and "k" of zero order equation were used as the dependent variables. The films were evaluated for mucoadhesive strength, in vitro residence time, swelling study, in vitro drug release, and effectiveness against Candida albicans. The concentration of poly(vinyl alcohol) and the number of freeze/thaw cycles both decrease the drug release rate. Mucoadhesive hydrogel film with 15% poly(vinyl alcohol) and 7 freeze/thaw cycles was optimized. The optimized batch exhibited the sustained release of drug and the antifungal studies revealed that the drug released from the film could inhibit the growth of Candida albicans for 12 hours.

摘要

制备并优化了用于口腔局部给药治疗口腔念珠菌病的粘膜粘附水凝胶膜。采用冻融交联技术，以聚乙烯醇制备粘膜粘附水凝胶膜。采用3(2)全因子设计优化配方。冻融循环次数(4、6和8次循环)和聚乙烯醇浓度(10%、15%和20%)作为自变量，而50%药物释放所需时间、第8小时药物释放累积百分比和零级方程的“k”作为因变量。对薄膜的粘膜粘附强度、体外停留时间、溶胀研究、体外药物释放以及对白色念珠菌的有效性进行了评估。聚乙烯醇浓度和冻融循环次数均降低了药物释放速率。优化了含15%聚乙烯醇和7次冻融循环的粘膜粘附水凝胶膜。优化后的批次表现出药物的持续释放，抗真菌研究表明，从薄膜中释放的药物可抑制白色念珠菌生长12小时。

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