RGD肽修饰的异长春花碱-粉防己碱脂质体的制备及体外抑瘤作用研究  

Preparation of Vinorelbine-tetrandrine Liposomes Modified with RGD and Study on the in vitro Antitumor Effect

作　　者：居瑞军[1] 王晓敏[2] 晁建平[1] 程岚[2] 李学涛[2] 

机构地区：[1]北京石油化工学院制药工程系,北京102617 [2]辽宁中医药大学药学院,辽宁大连116600

出　　处：《中国药房》2017年第25期3549-3552,共4页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81673603;81541081);辽宁省教育厅重点实验室基础研究项目(No.LZ2015053)

摘　　要：目的:制备RGD肽修饰的异长春花碱(VRB)-粉防己碱(TET)脂质体,研究其对脑胶质瘤C6细胞的抑制作用。方法:采用薄膜分散法和硫酸铵梯度法制备RGD肽修饰的VRB-TET脂质体,观察其形态和粒径分布,测定其中VRB的含量;以磺酰罗丹明B法分别测定空白靶向脂质体、VRB普通脂质体和RGD肽修饰的VRB-TET脂质体对C6细胞的抑制作用。结果:所制RGD肽修饰的VRB-TET脂质体呈圆球状或类圆球状,表面光滑,粒径为120 nm左右,其中VRB的平均含量为28.27μg/m L(RSD=0.38%,n=3)。空白靶向脂质体对C6细胞生长无显著影响;RGD肽修饰的VRB-TET脂质体能明显抑制C6细胞生长,其作用后细胞存活率明显低于VRB普通脂质体(P<0.05)。结论:成功制得RGD肽修饰的VRB-TET脂质体,其具有明显的抑制C6细胞生长的作用。OBJECTIVE： To prepare the vinorelbine-tetrandrine liposomes modified with RGD, and study the inhibitory effect on glioma C6 cells. METHODS： Film dispersion method and ammonium sulfate gradient method were used to prepare the vinorel- bine-tetrandrine liposomes modified with RGD, and the morphology and particle size distribution were observed. The vinorelbine content was determined, and sulforhodamine B method was used to respectively determine the inhibitory effects of blank targeting liposomes, normal vinorelbine liposomes and vinorelbine-tetrandrine liposomes modified with RGD on C6 cells. RESULTS： The prepared vinorelbine-tetrandrine liposomes modified with RGD were spherical or almost spherical with smooth surface, and particle size was about 120 nm. The average content of vinorelbine was 28.27 μg/mL （RSD=0.38%, n=3）. Blank targeting liposomes had no significant effect on the growth of C6 cells; vinorelbine-tetrandrine liposomes modified with RGD can obviously inhibit the growth of C6 cells, and cell viability after its effect was significantly lower than normal vinorelbine liposomes （P〈0.05）. CON- CLUSIONS： Vinorelbine-tetrandrine liposomes modified with RGD are successfully prepared, and they show obvious inhibitory ef- fects on the growth of C6 cells.

关 键 词：RGD肽 异长春花碱 粉防己碱 脂质体 体外抑瘤作用 

分 类 号：R943[医药卫生—药剂学] R979.1[医药卫生—药学]