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抗真菌药物克霉唑脂质体/非离子脂质体递送系统的制备及体外评价

Preparation and in vitro evaluation of liposomal/niosomal delivery systems for antifungal drug clotrimazole.

作者信息

Ning Meiying, Gu Zhongwei, Pan Huaizhong, Yu Heming, Xiao Kai

机构信息

Beijing Medical University, Beijing, China.

出版信息

Indian J Exp Biol. 2005 Feb;43(2):150-7.

Abstract

Clotrimazole, an imidazole derivative antifungal agent is widely used for the treatment of mycotic infections of the genitourinary tract. In order 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 regards to size and entrapment efficiency, multilamellar liposomes/niosomes containing drug were prepared by lipid hydration method. The ability of the systems to deliver clotrimazole into and through the mucosa was evaluated in vitro using rabbit vaginal mucosa with vertical Franz diffusion cells. The in vitro permeation data showed that the liposomes/niosomes system increased the clotrimazole total penetration through the vaginal mucosa by 1.6, 1.5-fold, the accumulation of clotrimazole into the mucosa was increased by 3.1, 2.3-fold, respectively, as compared with control during 24 hr. These results suggest that the studied liposomes/niosomes systems may be appropriate vesicles for the vaginal mucosa delivery of clotrimazole for local vaginal therapy.

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。为了开发克霉唑阴道给药的替代制剂,以提供用于局部阴道治疗的适当药物的持续和控释,脂质体/非离子型脂质体被评估为给药载体。为了在大小和包封率方面优化脂质体/非离子型脂质体的制备,通过脂质水化法制备了含药的多层脂质体/非离子型脂质体。使用带有垂直弗兰兹扩散池的兔阴道黏膜在体外评估该系统将克霉唑递送至黏膜并透过黏膜的能力。体外渗透数据显示,与对照相比,在24小时内,脂质体/非离子型脂质体系统使克霉唑透过阴道黏膜的总渗透量分别增加了1.6倍和1.5倍,克霉唑在黏膜中的蓄积量分别增加了3.1倍和2.3倍。这些结果表明,所研究的脂质体/非离子型脂质体系统可能是用于克霉唑阴道黏膜给药以进行局部阴道治疗的合适囊泡。

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