顺铂缓释多囊脂质体的制备和体外释放性能研究

目的 制备包封率高和缓释作用好的顺铂缓释多囊脂质体,并与反相蒸发法制备的顺铂普通脂质体比较其体外释药性能。方法 用复乳法制备顺铂多囊脂质体,非火焰原子吸收分光光度法测定顺铂含量,磷脂酶试剂法测定脂质体中磷脂的浓度。测定包封率和体外释药性。结果顺铂多囊脂质体平均粒径为16.6 μm,跨距为1.0。顺铂包封率可高达80%以上。顺铂缓释多囊脂质体的体外释药符合一级释药规律, 释药t_1/2为37.7 h,比反相蒸发法制备的顺铂普通脂质体延长8.4倍。经差示热分析发现辅助膜稳定剂有明显的膜稳定作用。结论顺铂多囊脂质体包封率高,并具有良好的缓释作用。

Preparation of cisplatin multivesicular liposomes and release of cisplatin from the liposomes in vitro

AIM: To prepare cisplatin multivesicular liposomes with high encapsulation efficiency and sustained-release character, and compare the release characteristics with conventional liposomes prepared by reverse-phase evaporation method. METHODS: Cisplatin multivesicular liposomes were prepared using multiple emulsion method. The concentrations of cisplatin and lipids in the liposomes were measured by flameless atomic absorbance spectroscopy (FAAS) and phosphalipid enzyme reagent method, respectively. The encapsulation efficiency, size and release of the cisplatin from the liposomes were studied in vitro. RESULTS: The mean diameter of cisplatin multivesicular liposomes was (16.6 +/- 1.0) micron. The encapsulation efficiency of cisplatin was more than 80%. The release profile in vitro fitted with a first-order equation. The releasing t1/2 of cisplatin multivesicular liposomes is 37.7 h, which is 8.4 that of conventional liposomes. Co-membrane stabilizer has remarkable stabilizing effect on the multivesicular liposomal membrane confirmed by differential scattering calorimetry (DSC). CONCLUSION: The cisplatin multivesicular liposomes showed high encapsulation efficiency and sustained-release character.