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.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
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)~~
关键词
线粒体靶向
聚合物
氯尼达明
三苯基膦
聚乙烯亚胺
mitochondria-targeted
polymer
lonidamine
triphenylphosphine
polyethyleneimine
