主动载药法制备硫酸卷曲霉素脂质体及其质量评价

Preparation of liposomes entrapped capreomycin sulfate by active loading and its quality evaluation

目的制备硫酸卷曲霉素脂质体,建立含量和包封率的测定方法,初步考察其体外释放规律。方法采用pH梯度法制备硫酸卷曲霉素脂质体,超滤法分离脂质体与游离药物,RP-HPLC测定脂质体的含量和包封率,透析法考察脂质体的体外释放行为。结果超滤法能很好地将脂质体与游离药物分离,测定硫酸卷曲霉素脂质体的含量为10.27mg/ml,包封率为47.8%,脂质体的体外释放规律符合一级动力学过程。结论pH梯度法适于制备硫酸卷曲霉素脂质体,超滤法可用于硫酸卷曲霉素脂质体包封率的测定,制备的脂质体具有一定的缓释效果。

Objective To prepare capreomycin sulfate liposomes to develop a method for determining its drug content and entrapment efficiency and to study the release profile in vitro. Methods Capreomycin sulfate was encapsulated into the liposomes using the pH gradient dependent remote loading technique. Free capreomycin sulfate and liposomes were separated by ultrafiltration, RP-HPLC was applied to determine the entrapment efficiency and dialysis was utilized to study the release behavior of drug from liposome in vitro. Results Free capreomycin sulfate and liposomes was well separated by ultrafiltration. The content and entrapment efficiency of capreomycin sulfate liposomes determined were 10. 27mg/ml and 47.8% respectively. The release profile in vitro was subjected to the first order model. Conclusion The pH gradient technique is suit- able for preparing capreomycin sulfate liposomes which exhibits sustained-release profile in vitro. Ultrafiltra- tion established in this study can be applied in the determination of entrapment efficiency of capreomycin sulfate liposomes.