替莫唑胺复方脂质体的制备及其体外抗肿瘤作用的评价  

Preparation of compound temozolomide liposomes and its anti-proliferation effect in vitro

作　　者：王亚华[1] 应雪[1] 轩亚茹 闫荷露 张春春[1] 李霞[1] 唐辉[1] 

机构地区：[1]新疆石河子大学药学院特种植物药资源教育部重点实验室,石河子832000

出　　处：《中国新药杂志》2016年第13期1511-1516,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金资助项目(81160396;81460540);石河子大学杰出青年科技人才培育计划项目(2012ZRKXJQ07);新疆生产建设兵团社会发展科技攻关与成果转化计划项目(2015AD007)

摘　　要：目的:研究替莫唑胺复方脂质体的制备工艺,并评价其体外抗肿瘤作用。方法:采用薄膜分散法制备复方脂质体,对处方进行优化;同时对脂质体进行粒径、Zeta电位表征;并采用磺酰罗丹明B蛋白(SRB)法考察脂质体对C6胶质瘤细胞的抗增殖作用。结果:采用最优处方,制备的复方脂质体中替莫唑胺和表没食子儿茶素没食子酸酯的包封率分别为(20.87±0.22)%和(85.86±0.31)%;平均粒径和Zeta电位分别为(170.1±0.42)nm和(-8.22±0.66)mV;制备得到的复方脂质体对C6细胞具用较强的抑制作用。结论:本方法制备的脂质体方法简单,粒径均一,且体外抗肿瘤作用强。Objective： To investigate the preparation technology of compound temozolomide liposomes,and its anti-tumor effect in vitro. Methods： The compound temozolomide liposomes were prepared by thin film dispersion method and the formulation was optimized. The particle size and Zeta potential of liposomes were characterized.The anti-proliferation effect of the liposomes on C6 glioma cells was investigated by the method of sulforhodamine B（ SRB）. Results： The encapsulation efficiencies were（ 20. 87 ± 0. 22） % and（ 85. 86 ± 0. 31） % for temozolomide and EGCG,respectively,detected by HPLC. The average particle size and Zeta potential were（ 170. 1 ± 0. 42） nm and（- 8. 22 ± 0. 66） m V,and the compound temozolomide liposomes had strong inhibiting effect in C6 cells.Conclusion： The optimal preparation method of compound temozolomide liposomes is simple,the particle size is uniform,and the antitumor effect in vitro is strong.

关 键 词：替莫唑胺 复方脂质体 高效液相色谱法 处方优化 包封率 体外抗肿瘤作用 

分 类 号：R979.1[医药卫生—药品]