一种肿瘤与热双重靶向的异丙基丙烯酰胺胶束的制备、表征与体内应用  

Preparation,charaterization and in vivo application of tumor and thermal dual-targeting isopropyl acrylamide micell

作　　者：金靖[1] 陈海燕[1] 田俊梅[1] 崔思思[1] 李洋[1] 顾月清[1] 

机构地区：[1]中国药科大学生命科学与技术学院生物医学工程研究室,南京210009

出　　处：《科学通报》2013年第7期545-555,共11页Chinese Science Bulletin

基　　金：国家自然科学基金(81220108012;81211140243;30970776;81000666;81071194;81171395)资助

摘　　要：利用自由基随机共聚反应原理,合成了P(FAAn-co-NIPA-co-AAm-co-ODA)聚合物,该聚合物兼具温度响应性和叶酸介导肿瘤主动靶向能力,并在水中自主装形成胶束.通过紫外光谱、红外光谱、核磁共振谱对聚合物的结构、胶束的临界相变温度(LCST)及水合粒径进行了考察,并利用透射电子显微镜考察胶束的粒径及形貌.胶束粒径为80nm,LCST为43℃.MTT实验结果显示,胶束载体对A549和Bel-7402肿瘤细胞基本无毒性.装载近红外荧光探针(ICG-Der-01)的胶束在MDA-MB-231和HCT116荷瘤裸鼠体内的动态分布研究证实,该胶束载体具有明显的叶酸靶向能力与热靶向能力.The polymers containing folate, isopropyl acrylamide and octadecyl acrylate were formed through free radical random copolymerization, and then micells were formed in aqueous solution by self assembly. The micelles were provided with the advantages of temperature sensitivity and active tumor targeting capability. The micells were characterized by UV-vis spectra, FTIR spectra, NMR spectra, lower critical solution temprature （LCST） and TEM. The size and LCST of the micelles were 80 nm and 43℃, respectively. MTT assays demonstrated the low biotoxicity of the micelles on A549 cells and Bel 7402 cells. The in vivo experiments verified the dual tumor-targeting efficacy of the micells based on MDA-MB-231 and HCT 116 tumor-beard mice models.

关 键 词：异丙基丙烯酰胺 胶束 叶酸 温度敏感性 肿瘤靶向 热靶向 

分 类 号：O623.7[理学—有机化学]