多西紫杉醇纳米脂质体的制备及性质考察

Preparation and characterization of docetaxel nanoliposomes

目的制备多西紫杉醇纳米脂质体,并考察其理化性质和体外释药行为。方法采用薄膜分散-高压均质法制备多西紫杉醇纳米脂质体,单因素考察法优化处方。透射电镜观察脂质体的形态,动态激光散射法测定粒径分布、Zeta电位,反透析法测定包封率,动态膜透析法考察体外释药行为。结果最佳处方为:药脂比1∶15,胆固醇、磷脂质量比1∶8,有机相/水相比例为5∶1。优化条件下制备的多西紫杉醇脂质体的粒径为(200.3±3.7)nm,Zeta电位-15.10 m V,包封率为(90.76±1.42)﹪,体外释放符合Higuchi方程。结论制备的多西紫杉醇脂质体粒径均匀、包封率高,优化的处方工艺可行。

Objective： OBJECTIVE To prepare docetaxel nanoliposomes and investigate their physico-chemical properties and release profile in vitro. Methods： Docetaxel liposomes were prepared by film dispersion-high pressure homogenization technology. The formulation was optimized using single factor screening. Transmission electron microscopy was used to study the shape. The diameter and Zeta potential was measured by dynamic light scattering. Retrodialysis method was used to determine the entrapment efficiency of the liposomes. In vitro drug release of the liposomes was investigated using dialysis method. Results： TS The optimized formulation was as follows： m（ drug） ∶ m（ lipids） = 1∶ 15,m（ cholesterol） ：m（ soya lecithin） = 1 ∶ 8,organic phase / aqueous solution ratio was 5 ∶ 1. The mean diameter of the liposomes was（ 200. 3 ± 3. 7） nm with Zeta potential of-15. 10 m V,and the entrapment efficiency was（ 90. 76 ± 1. 42） ﹪. The in vitro drug release profile was fitted with Higuchi equation. Conclusion： The uniform nanoliposomes with high entrapment efficiency indicated the optimized formulation was feasible.