异长春花碱脂质体的制备及理化性质研究

Preparation and Physicochemical Properties of Vinorelbine Liposomes

目的:制备异长春花碱脂质体,并考察其理化性质。方法:采用薄膜分散法制备异长春花碱脂质体;透射电镜下观察脂质体外观形态,激光散射法测定脂质体粒径分布和Zeta表面电位,葡聚糖凝胶法分离脂质体与未包封的药物以测定脂质体的包封率和渗漏率,膜动态透析法探讨脂质体的体外释药特性。结果:异长春花碱脂质体平均粒径149.2 nm,透射电镜可以明显观察出脂质体的双分子层结构,Zeta电位为38.62 mv,包封率均大于85%(n=3),冰箱(<4℃)保存9个月后脂质体的渗漏率小于9.0%,脂质体体外释放可延长至24 h,释放规律符合Higuchi方程。结论:所制备的异长春花碱脂质体粒径均匀,外观良好,包封率高,体外释药具有明显的缓释效果。

Objective：To prepare the vinorelbine liposomes and investigate their physicochemical properties. Methods：Vinorelbine liposomes were prepared by thin-film ultrasonication method. The morphology of the liposomes was detected by transmission electron microscopy. The partical size distribution and zeta potential were investigated by laser scattering. Sephadex 0-50 was applied to sepa- rate the free drug and liposomes in order to determine the entrapment efficiency and leakage efficiency of the liposomes. The release characteristics of vinorelbine liposomes were measured by dialysis method. Results：The particle size of the liposome was 149. 2 nm, the bilayer of the liposome was observed obviously. The zeta potential was 38. 62 my. The entrapment efficiency of vinorelbine liposomes was more than 85% （n = 3）, and the leakage efficiency was less than 9. 0% preserved in refrigerator（ 〈 4~C ）. In vitro release test, it could sustain for 24h and conform to the Higuchi model. Conclusion ： The vinorelbine liposomes have uniform partical size, fine-looking, high entrapment efficiency and sustained releasing effect.