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克霉唑脂质体/非离子表面活性剂囊泡凝胶递送系统的制备、体外和体内评价

Preparation, in vitro and in vivo evaluation of liposomal/niosomal gel delivery systems for clotrimazole.

作者信息

Ning Meiying, Guo Yingzhi, Pan Huaizhong, Chen Xianli, Gu Zhongwei

机构信息

Centre of Drug Controlled Release Research, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China.

出版信息

Drug Dev Ind Pharm. 2005 May;31(4-5):375-83. doi: 10.1081/ddc-54315.

Abstract

Clotrimazole, which is an imidazole derivative antifungal agent, was widely used for the treatment of mycotic infections of the genitourinary tract. To develop alternative formulation for the vaginal administration of clotrimazole to provide sustained and controlled release of appropriate drug for local vaginal therapy, liposomes/niosomes were evaluated as delivery vehicles. To optimize the preparation of liposomes/niosomes with regard to size and entrapment efficiency, multilamellar liposomes/niosomes containing drug were prepared by lipid hydration method. The prepared liposomes/niosomes were incorporated into 2% carbopol gel, and the systems were evaluated for drug stability in phosphate-buffered saline (pH 7.4) and simulated vaginal fluid at 37 +/- 1 degrees C. Further, the vesicle gel system was evaluated by antifungal activity and tolerability on tissue level in rat.

摘要

克霉唑是一种咪唑衍生物抗真菌剂,广泛用于治疗泌尿生殖道真菌感染。为开发克霉唑阴道给药的替代制剂,以实现局部阴道治疗药物的持续和控释,对脂质体/非离子型脂质体作为给药载体进行了评估。为在尺寸和包封率方面优化脂质体/非离子型脂质体的制备,采用脂质水化法制备了含药的多层脂质体/非离子型脂质体。将制备的脂质体/非离子型脂质体加入到2%卡波姆凝胶中,并在37±1℃下于磷酸盐缓冲液(pH 7.4)和模拟阴道液中对该体系进行药物稳定性评估。此外,通过大鼠组织水平的抗真菌活性和耐受性对囊泡凝胶体系进行了评估。

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