西妥昔单抗修饰异长春花碱隐形阳离子脂质体的制备及其理化性质、细胞抑制作用研究  

Study on Preparation,Physicochemical Properties and Cell Inhibition of IMC-C225 Modified Vinorelbine Stealth Cationic Liposomes

作　　者：林祥辉 王晓敏[2] 王艳红[2] 李学涛[2] 

机构地区：[1]临沂经济技术开发区人民医院药剂科,山东临沂276023 [2]辽宁中医药大学药学院,辽宁大连116600

出　　处：《中国药房》2016年第28期3964-3967,共4页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81541081);辽宁省科学技术计划项目(No.2014020046);辽宁省教育厅重点实验室基础研究项目(No.LZ2015053)

摘　　要：目的:制备西妥昔单抗(IMC-C225)修饰异长春花碱(VRB)隐形阳离子脂质体(以下简称VRB阳离子脂质体),并对其理化性质和细胞抑制作用进行研究。方法:采用硫酸铵梯度法制备VRB阳离子脂质体,同时对VRB阳离子脂质体的形态学、粒径、多分散系数(PDI)、Zeta电位、包封率、体外释放度等理化性质进行研究,采用磺酰罗丹明B(SRB)法检测VRB阳离子脂质体对肺癌Lewis细胞的抑制作用。结果:所制备的VRB阳离子脂质体外观呈圆球形、大小均匀、表面光滑,平均粒径为(89.06±3.56)nm,PDI为0.175±0.01,Zeta电位为(35.91±0.51)m V,包封率为(90.61±0.80)%,48 h的体外释放度为(26.74±3.76)%(n=3);与异长春花碱脂质体和IMC-C225修饰空白隐形阳离子脂质体比较,VRB阳离子脂质体能降低Lewis细胞的存活率。结论:所制备的VRB阳离子脂质体粒径均匀、包封率较高,对Lewis细胞有明显的抑制作用。OBJECTIVE： To prepare IMC-C225 modified vinorelbine （VRB） stealth cationic liposomes （called VRB cationic li- posomes for short）, and to study the physicochemical properties and cell inhibition. METHODS： The VRB cationic liposomes were prepared by ammonium sulfate gradient method. The physicochemical properties, including morphology, particle size, polydispersi- ty index （PDI）, Zeta potential, encapsulation efficiency and in vitro release rate, were studied. The inhibitory effects of the liposomes on lung caner Lewis cell were evaluated by SRB methods. RESULTS： The prepared VRB cationic liposomes were spheroidal in shape, even in size and smooth in surface. The average particle size of liposomes was （89.06 ± 3.56） nm, PDI value was 0.175± 0.01 and Zeta potential was （35.91 ±0.51） mV. The encapsulation efficiency was （90.61 ± 0.80）%, and in vitro release rate was （26.74 ± 3.76）% within 48 h （n=3）. Compared with vinorelbine liposomes and IMC-C225 modified blank stealth cationic liposomes, VRB cationic liposomes could reduce the survival rate of Lewis cells. CONCLUSIONS： Prepared VRB cationic liposomes have even particle size and high encapsulation efficiency, and show significant inhibitory effect on Lewis cells.

关 键 词：异长春花碱 西妥昔单抗 隐形阳离子 脂质体 理化性质 细胞抑制 

分 类 号：R943[医药卫生—药剂学]