转铁蛋白与RGD共修饰脂质体用于脑胶质瘤靶向性研究  

Liposome modified by transferrin and RGD for glioma targeting

作　　者：邵云[1] 俞向荣[1] 吴一平[1] 姚建社[1] 羊正祥[1] 

机构地区：[1]无锡市人民医院神经外科,江苏无锡214023

出　　处：《第三军医大学学报》2014年第6期592-595,共4页Journal of Third Military Medical University

摘　　要：目的构建转铁蛋白与整合素受体精氨酸-甘氨酸-天冬氨酸(Arg-Gly-Asp,RGD)三肽序列共修饰脂质体,并对其脑胶质瘤靶向性进行初步研究。方法采用薄膜分散法制备RGD修饰脂质体,采用后插入法制备转铁蛋白与RGD共修饰脂质体,观察其形态、粒径、电位。通过U87脑胶质瘤细胞摄取实验以及裸鼠脑组织离体成像实验考察脂质体的脑胶质瘤靶向性。结果所制备的双配体脂质体粒径在RGD/TF-LP为(120.0±8.5)nm,电位为(-5.00±1.15)mV。体外细胞摄取实验表明,U87脑胶质瘤细胞对共修饰脂质体的摄取效率分别是转铁蛋白修饰脂质体和RGD修饰脂质体的2.1倍和2.7倍。肿瘤球摄取实验以及裸鼠脑组织离体成像实验表明共修饰脂质体具有良好的肿瘤靶向性以及脑部肿瘤传递能力。结论转铁蛋白与RGD共修饰脂质体具有一定的脑胶质瘤靶向性,是一种潜在的脑胶质瘤给药系统。Objective To prepare liposomes co-modified by transferrin and Arg-Gly-Asp （RGD） and to evaluate their glioma-targeting efficiency in vitro and in vivo. Methods The co-modified liposome was prepared by film-ultrasonic method. The appearance, particle size, and Zeta potential were evaluated. The cellular uptake by U87 cells in vitro and in vivo imaging were used to evaluate the targeting efficiency. Results The particle diameter of the co-modified liposome was 120.0 ± 8.5 nm with the Zeta potential of - 5.00 ± 1.15 inV. The results demonstrated that the co-modified liposome uptaken by U87 were 2.1 and 2.7 times higher than that of transferrin-modified liposome and RGD-modified liposome, respectively. The evaluation of tumor spheroid penetration and in vivo imaging showed the co-modified liposome had the strongest fluorescence intensity. Conclusion The co-modified liposome might serve as a promising glioma delivery system of antitumor drugs.

关 键 词：转铁蛋白 精氨酸 甘氨酸 天冬氨酸三肽序列 脂质体 脑胶质瘤 

分 类 号：R341[医药卫生—基础医学] R394-33