Pavelić Z, Skalko-Basnet N, Jalsenjak I
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Eur J Pharm Sci. 1999 Aug;8(4):345-51. doi: 10.1016/s0928-0987(99)00033-0.
To develop a novel vaginal delivery system, able to effectively deliver entrapped drugs during an extended period of time at the site of action, liposomes made of phosphatidylcholine were prepared by two different methods, namely the polyol dilution method and the proliposome method. Liposomes containing three commonly applied drugs in the treatment of vaginal infections: clotrimazole, metronidazole and chloramphenicol were tested for in vitro stability (in buffers at pH 4.5 and 5.9 representing pre- and postmenopausal vaginal pH). In situ stability (in the presence of cow vaginal mucosa) showed that after 6 h incubation (at 37 degrees C), liposomes retained more than 40% of originally entrapped clotrimazole, 28% of entrapped metronidazole or 37% of entrapped chloramphenicol. In vitro and in situ stability studies confirmed the applicability of liposomes as a carrier system for vaginal delivery. Even after 24 h of incubation in the presence of vaginal mucosa liposomes retained sufficient amounts of entrapped drugs.
为开发一种新型阴道给药系统，使其能够在作用部位长时间有效递送包裹的药物，采用两种不同方法制备了由磷脂酰胆碱制成的脂质体，即多元醇稀释法和前体脂质体法。对含有三种治疗阴道感染常用药物（克霉唑、甲硝唑和氯霉素）的脂质体进行了体外稳定性测试（在pH值为4.5和5.9的缓冲液中，分别代表绝经前和绝经后阴道pH值）。原位稳定性（在牛阴道黏膜存在下）表明，孵育6小时（37℃）后，脂质体保留了超过40%最初包裹的克霉唑、28%包裹的甲硝唑或37%包裹的氯霉素。体外和原位稳定性研究证实了脂质体作为阴道给药载体系统的适用性。即使在阴道黏膜存在下孵育24小时后，脂质体仍保留了足够量的包裹药物。
