线粒体靶向聚合物TPP-PEI-LND的构建及其特性  

Construction and characterization of mitochondria-targeted TPP-PEI-LND

作　　者：张兵锋[1,2] 姜虎林 

机构地区：[1]中国药科大学药学院,南京210009 [2]贵阳中医学院,贵阳550002

出　　处：《中国药科大学学报》2015年第6期659-664,共6页Journal of China Pharmaceutical University

基　　金：江苏省自然科学基金资助项目(No.BK20140659)~~

摘　　要：以低相对分子质量聚乙烯亚胺（PEI）为骨架将线粒体靶向基团三苯基麟（TPP）和化疗药物氯尼达明（LND）以酰胺键接枝到PEI上,构建线粒体靶向聚合物TPP-PEI-LND。TPP-PEI-LND经^1H NMR确证。采用透析法考察TPP-PEILND的体外释放。采用HeLa细胞研究TPP-PEI-LND的线粒体靶向能力和细胞毒性。结果显示,TPP-PEI-LND线粒体靶向聚合物制备成功,其释药行为呈现缓释特点,并可以靶向递送药物到达线粒体,显著增强药物对肿瘤细胞的疗效。The mitochondria-targeted TPP-PEI-LND was synthesized by mitochondria-targeted ligand triphenylphosphine （TPP） and therapeutic drug lonidamine （LND） conjugated to low molecular weight branched polyethyleneimine （PEI）. TPP-PEI-LND was verified using 1H NMR; in vitro release was determined by the dialysis. Besides, the cytotoxicity and mitochondria-targeted potential of TPP-PEI-LND were investigated in HeLa cells. The results showed that TPP-PEI-LND was successfully synthesized and it exhibited the feature of extended- release. Hence, TPP-PEI-LND could deliver LND to mitochondria, resulting in significantly enhanced efficacy of LND.

关 键 词：线粒体靶向 聚合物 氯尼达明 三苯基膦 聚乙烯亚胺 

分 类 号：R943[医药卫生—药剂学]