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仿红细胞膜质体的研究

侯新朴, 仇勇, 张俊梅   

  1. 北京医科大学药学院, 北京 100083
  • 收稿日期:1996-11-20 修回日期:1997-07-07 出版日期:1997-12-15 发布日期:1997-12-15

Study on Liposomes of Mimetic Red Cell

Xin-Pu Hou, Yong Qiu, Jun-Mei Zhang   

  1. School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083
  • Received:1996-11-20 Revised:1997-07-07 Online:1997-12-15 Published:1997-12-15

摘要: 本项研究从仿红细胞出发, 将增加双分子脂膜亲水性的PEG-PE(聚乙二醇与磷脂酰乙醇胺的衍生物)及增加双分子脂膜硬度的SM(神经鞘磷脂)掺入脂质体, 比较其在体外稳定性、体内分布及清除半衰期。结果证明该类脂质体稳定性提高, 体内被肝、脾清除减少, 血循环中半衰期显著延长。本研究为脂质体载药至非网状内皮系统的靶向给药打下基础。

关键词: 脂质体, 亲水性修饰, 硬度修饰

Abstract: Liposomes were prepared by adding hydrophilic agents PEG-PE, rigidity agent SM in the bilayer membrane for mimetic red cell membrane. In PBS or serum, release of calcein content from liposomes dramatically decreased, which demonstrated increasing membrane stability by adding PEG-PE or SM. The ratio b/R of the remains of liposomes in blood to that in RES was used as a parameter of biodistribution in vivo. At 2 h after iv injection, b/R of modified liposomes was enhanced 6.5~13.1 fold. Their clearance half-life from blood circulation was delayed 1.6~5.8 fold. The modification of liposome membrane by PEG-PE or SM is the favorable condition for drug-liposomes to target the non-RES.

Key words: Liposomes, Hydrophilic modification, Rigidity modification

Supporting: *Supported by National Natural Science Foundation of China.