TPGS修饰青蒿琥酯脂质体的制备及其体外抗肿瘤活性  

Preparation of TPGS-modified artesunate liposomes and their in vitro anti-tumor activity

作　　者：胡诚[1] 梁琨[1] 安叡[1] 王新宏[1] 尤丽莎[1] HU Cheng LIANG Kun AN Rui WANG Xin-hong YOU Li-sha(Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China)

机构地区：[1]上海中医药大学,上海201203

出　　处：《中成药》2017年第3期492-498,共7页Chinese Traditional Patent Medicine

摘　　要：目的制备聚乙二醇1000维生素E琥珀酸酯(TPGS)修饰青蒿琥酯脂质体,并考察其体外抗肿瘤活性。方法薄膜分散法制备脂质体,透射电镜和粒径仪进行表征,超滤离心法测定包封率。MTT法评价其对人肝癌HepG2细胞的毒活性。结果所得脂质体平均粒径126.7 nm,PDI 0.182,Zeta电位-10.1 mV,包封率78.8%,载药量18.38%。其对HepG2细胞具有明显抑制作用,IC_(50)为0.034μmol/mL。结论与TPGS未修饰青蒿琥酯脂质体相比,该方法制备的TPGS修饰青蒿琥酯脂质体粒径更小,稳定性更好,包封率更高,而且具有更强的体外抗肿瘤活性。AIM To prepare D-α-tocopherol polyethylene glycol 1000 succinate（TPGS）-modified artesunate liposomes and to investigate the in vitro anti-tumor activity.METHODS The liposomes prepared by thin-film dispersion method were characterized by transmission electron microscopy and particle size analyzer,and the encapsulation efficiency was determined by ultrafiltration centrifugation.The liposomes’ cytotoxicity to human hepatoma HepG2 cells was evaluated by MTT method.RESULTS The average particle size,PDI,Zeta potential,encapsulation efficiency,drug loading of the liposomes were 126.7 nm,0.182,-10.1 mV,78.8% and 18.38%,respectively.The liposomes displayed a significant inhibition on HepG2 cells with the IC50 value of 0.034 μmol/mL.CONCLUSION Compared with non-TPGS-modified artesunate liposomes,the TPGS-modified artesunate liposomes prepared by this method afford smaller vesicle size,better stability and higher encapsulation efficiency with stronger in vitro anti-tumor activity.

关 键 词：青蒿琥酯 脂质体 聚乙二醇1000维生素E琥珀酸酯(TPGS) 制备 体外抗肿瘤活性 人肝癌HEPG2细胞 

分 类 号：R943[医药卫生—药剂学]