摘要
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。
Objective To optimize the formulation of long-circulating cationic teniposide-containing liposomes.Methods The long-circulating cationic teniposide-containing liposomes were prepared by thin film dispersion method.Single factor experiment and orthogonal design were adopted to screen the formulation.Results The ideal combination of formulation was as follows：DSPC-PEG5 000-DOTMA（4∶1）;teniposide-phospholipid（1∶4）;phospholipid-cholesterol（2∶1）;lecithin as an emulsifier with purity of80%.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 teniposide-containing liposomes were quite stable after being stored in 5±3 ℃ for 180 dand 25±2 ℃ for 30 d.Conclusion The optimized,sustained release long-circulating cationic teniposide-containing liposomes with satisfied size and high entrapment efficiency were obtained,which was safe and stable.
出处
《西北药学杂志》
CAS
2017年第6期771-774,共4页
Northwest Pharmaceutical Journal
关键词
替尼泊苷
长循环阳离子脂质体
薄膜分散法
磷脂
卵磷脂
胆固醇
teniposide
long-circulating cationic teniposide-containing liposomes
thin film dispersion method
phospholipid
lecithin
cholesterol
