利福平脂质体温敏型原位凝胶的制备及其体外释药特征研究

Preparation of Rifampicin Liposomes in Situ Gel System and Its in Vitro Release Mechanism

关键词:  利福平  脂质体  温敏型原位凝胶  溶蚀

Key words:  rifampicin  liposomes  in situ gel system  erosion

摘要:

目的 制备利福平脂质体温敏型原位凝胶，并对其体外性质进行研究。方法 采用薄膜分散法制备利福平脂质体，并对利福平脂质体进行表征研究；以泊洛沙姆188、泊洛沙姆407为凝胶基质，制备利福平脂质体温敏型原位凝胶；以无膜溶出模型研究温敏型原位凝胶体外累积溶蚀率；采用透析袋法分析药物体外释放情况。结果 制备的利福平脂质体平均粒径、聚分散指数、Zeta电位、包封率和载药量分别为(149.0±5.67)nm、0.275±0.056、-(29.8±1.59)mv、(79.6±2.67)%，(18.6±0.25)%；利福平脂质体温敏型原位凝胶的胶凝温度为(34.3±0.6)℃。体外溶蚀曲线和体外释药曲线均符合零级动力学特征。结论 利福平脂质体温敏型原位凝胶的制备工艺简单易行，体外释放显示其有很好的缓释作用。

Abstract:

OBJECTIVE To prepare temperature sensitive in situ gel of rifampicin liposomes, and study its in vitro properties. METHODS Rifampicin liposomes were prepared by film dispersion method, further, its characteristics were investigated; poloxamer 188 and poloxamer 407 were used as gel base material to prepare temperature sensitive in situ gel of rifampicin liposome. A membraneless dissolution model was used to determine gel erosion of rifampicin in situ gel system. RESULTS The zeta potential, dispersion index, the mean particle size, entrapment efficiency, drug loading of liposomes was (149.0±5.67)nm, 0.275±0.056, -(29.8±1.59)mv, (79.6±2.67)%, (18.6±0.25)%, respectively. Gel temperature of rifampicin liposomes in situ gel system was (34.3±0.6)℃. The in vitro gel erosion behavior and release behavior of the rifampicin liposomes in situ gel system exhibited the characteristics of zero order kinetics. CONCLUSION It is easy to prepare rifampicin liposomes in situ gel system with suitable formulation. The release of the rifampicin liposomes in situ gel system shows good sustained release effect in vitro.