Ning M, Guo Y, Pan H, Zong S, Gu Z
Chinese Academy of Medical Science & Peking Union Medical College, Beijing, P.R. China.
Pharmazie. 2006 Mar;61(3):208-12.
Clotrimazole, an imidazole derivative antifungal agent, has been widely used for the treatment of mycotic infections of the genitourinary tract. In order to develop alternative formulations for the vaginal administration of clotrimazole which would provide sustained and controlled release of the appropriate drug for local vaginal therapy, liposomes/niosomes were evaluated as delivery vehicles. To optimize the preparation of the liposomes/niosomes with regard to size and entrapment efficiency, multilamellar liposomes/ niosomes containing the drug were prepared by a lipid hydration method. The liposomes/niosomes thus prepared were evaluated for their stability as drug-loaded liposomes/niosomes in simulated vaginal fluid at 37 +/- 1 degrees C. The two vesicle systems were also evaluated with regard to rat and rabbit vaginal irritation.
克霉唑是一种咪唑衍生物抗真菌剂,已被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,以实现局部阴道治疗所需药物的持续和控释,对脂质体/非离子型脂质体作为给药载体进行了评估。为了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。将如此制备的脂质体/非离子型脂质体作为载药脂质体/非离子型脂质体在37±1℃的模拟阴道液中评估其稳定性。还对这两种囊泡系统进行了大鼠和兔阴道刺激性评估。