抗VEGF单克隆抗体偶联5-FU纳米微粒的初步研究  

The anti VEGF monoclonal antibody conjugated with nanometer particle of 5-FU

作　　者：黄开红[1] 王凌云[1] 赵晓龙[1] 刘建化[1] 陈汝福[2] 朱兆华[1] 

机构地区：[1]中山大学附属第二医院消化内科,广东广州510120 [2]中山大学附属第二医院普通外科,广东广州510120

出　　处：《中国病理生理杂志》2007年第2期258-261,共4页Chinese Journal of Pathophysiology

基　　金：广州市科技攻关项目资助(No.2003Z3-E0351)

摘　　要：目的:为了提高5-氟尿嘧啶(5-fluorouracil,5-FU)的抗癌活性,采用抗VEGF单克隆抗体与5-FU聚乳酸纳米微粒交联结合制备具有靶向功能的免疫纳米微粒。方法:采用抗VEGF单克隆抗体与已制备的5-FU聚乳酸纳米微粒(5-FU-NPs)以化学键偶联连接的方法制备具有靶向功能的5-FU免疫纳米微粒(5-FU-Ab-NPs),考察其形貌、粒径分布、体外释放和免疫活性等性能。结果:5-FU-Ab-NPs仍呈规则球形,粒径约为(202±23)nm,体外释放实验表明该5-FU-Ab-NPs与5-FU-NPs具有相似缓释特性,免疫学检测和电镜检视显示偶联后的抗VEGF单克隆抗体免疫活性保持原活性的80%以上。结论:5-FU-Ab-NPs保持原5-FU-NPs缓释药物的特点,具有双重活性功能,即免疫导向和缓释药物,有利于提高肿瘤局部药物浓度。AIM： The characteristics of nanometer particles, which were prepared by the conjugation of anti - VEGF monoclonal antibodies and 5 -fluorouracil -loaded polylactic acid nanometer particles （5 - FU - NPs）, were investigated for improving the anticancer activity of 5 - FU. METHODS ： The method of couple linkage of chemical bonds was used to prepare the 5 -FU- NPs with VEGF antibody, then the appearance, distribution of particle diameter, releasing in vitro and the immunological activity were detected. RESULTS： The 5 - FU - Ab - NPs appeared as regular globular, the average particle diameter was （202 ±23 ）nm. The 5 -FU -Ab- NPs possessed the similar delayed release character of 5 - FUs. More than 80% of the immmunogical activity were detected in conjugates- retained antibody by the immunological methods and electron microscopy. CONCLUSION： The 5 - FU - Ab - NPs possess the similar delayed released activity to 5 - FU - NPs and have double activity of immune targeting and delayed releasing, which may increase the local concentration of 5 - FU.

关 键 词：氟尿嘧啶 抗VEGF单克隆抗体 免疫纳米微粒 胃肿瘤 MGC803细胞 

分 类 号：R944[医药卫生—药剂学]