替尼泊苷长循环阳离子脂质体的制备

目的优化薄膜分散法制备替尼泊苷长循环阳离子脂质体的最佳处方。方法薄膜分散法制备脂质体,以粒径和包封率为考察指标,用单因素考察和正交设计等方法优化脂质体的处方。结果优化后的最佳处方为:磷脂DSPC和PEG 5 000-DOTMA比为4∶1,药物和磷脂比为1∶4,磷脂与胆固醇比为2∶1,乳化剂为卵磷脂。优化的脂质体平均粒径为115.45nm,平均Zeta电位为25.54mV,平均包封率为91.32%,5±3℃放置180d和25±2℃放置30d各项指标变化不显著。结论制备的替尼泊苷长循环阳离子脂质体包封率高,粒径小,释放缓慢,稳定性和安全性好。

Preparation of long-circulating cationic teniposide-containing liposomes

Objective To optimize the formulation of long-circulating cationic teniposide-containing liposomes .Methods The long-cir-culating cationic teniposide-containing liposomes were prepared by thin film dispersion method .Single factor experiment and or-thogonal design were adopted to screen the formulation .Results The ideal combination of formulation was as follows :DSPC-PEG 5000-DOTMA (4:1);teniposide-phospholipid (1:4);phospholipid-cholesterol (2:1);lecithin as an emulsifier with purity of 80% .The average particle size of the optimized long-circulating cationic teniposide-containing liposomes was 115 .45 nm (n=3) , and the average Zeta potential was 25 .54 mV (n=3) ,and the average encapsulation efficiency was 91 .32% (n=3) .The tenipo-side-containing liposomes were quite stable after being stored in 5 ± 3 ℃ for 180 d and 25 ± 2 ℃ for 30 d .Conclusion The opti-mized ,sustained release long-circulating cationic teniposide-containing liposomes with satisfied size and high entrapment efficiency were obtained ,which was safe and stable .