维生素A修饰的阿霉素隐形脂质体对肝星状细胞的靶向性  

Study on the targeting ability of vitamin A-modified stealth liposomes encapsulating doxorubicin to hepatic stellate cells

作　　者：杨爱华[1] 张华[1] 章俊麟[1] 金武[1] 王学清[1] 张强[1] 

机构地区：[1]北京大学药学院药剂学系,北京100191

出　　处：《中国新药杂志》2013年第15期1797-1801,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(81273456;81130059)

摘　　要：目的:制备维生素A(VA)修饰的阿霉素隐形脂质体,考察其对肝星状细胞(HSC)的靶向性。方法:采用前插法和后插法优化VA修饰的阿霉素隐形脂质体的处方和工艺;采用流式细胞术对所得脂质体进行靶向性考察。结果:后插法中VA的加入量最高可以达卵磷脂的282%,包封率在90%以上;前插法VA的加入量只能达到卵磷脂的0.147%,包封率在80%左右。与普通的阿霉素隐形脂质体相比,VA修饰的阿霉素隐形脂质体对HSC-T6细胞具有更好的靶向性。当VA与EPC摩尔比为1∶2时,VA修饰的阿霉素隐形脂质体可被HSC-T6最大程度地摄取。结论:VA修饰的阿霉素隐形脂质体具有良好的HSC-T6细胞靶向性。Objective： To prepare vitamin A （VA）-modified stealth liposomes encapsulating doxorubicin and evaluate their possibility to target hepatic stellate cell （HSC）. Methods： Pre-inserting and post-inserting methods were used to prepare VA-modified liposomes encapsulating doxorubicin, and the targeting character of the liposomes was determined by flow cytometry. Results： The VA amount for post-inserting method could reach 282% of EPC and the entrapment efficiency was more than 90% ; while for pre-inserting method, the VA amount was only 0. 147% of EPC and the entrapment efficiency was around 80%. The targeting analysis data showed that the VA- modified stealth liposomes had higher targeting ability to HSC-T6 cells than that of conventional stealth liposomes, and the best VA to EPC mol ratio was 1：2. Conclusion： VA-modified stealth liposomes have good targeting ability to hepatic stellate cells.

关 键 词：隐形脂质体 维生素A 肝星状细胞 阿霉素 

分 类 号：R943[医药卫生—药剂学]