含磷脂胆碱仿生结构的阳离子聚合物胶束用作药物载体  

Cationic Polymer Micelles Containing Phosphatidylcholine Biomimetic Structure as Drug Carriers

作　　者：汪权 雷栋钦 孔越 罗祥林 Quan Wang;Dongqin Lei;Yue Kong;Xianglin Luo(College of Polymer Science and Engineering,Sichuan University,Chengdu 610065,China;State Key Laboratory of Colyger Materials CnEgminn,CiennSu 610065,Ciina)

机构地区：[1]四川大学高分子科学与工程学院 [2]高分子材料工程国家重点实验室(四川大学),四川成都610065

出　　处：《高分子材料科学与工程》2019年第7期1-8,共8页Polymer Materials Science & Engineering

基　　金：国家自然科学基金资助项目(51673129)

摘　　要：通过点击反应与ATRP反应合成了含有磷脂胆碱仿生结构的阳离子聚合物——聚{α-[4-(二乙氨基)甲基-1,2,3-三唑]-己内酯-co-己内酯}-b-聚(2-甲基丙烯酰氧基乙基磷酰胆碱)(PDCL-PMPC)。用核磁共振、红外、差示扫描量热分析确证了聚合物的结构。动态光散射法与透射电镜结果显示,该材料在水中能自组装形成粒径120 nm左右的球形胶束。研究发现,该聚合物胶束对超疏水的阴离子药物氯尼达明(LDN)有较高的包载量。体外MTT实验证明,PDCL-PMPC胶束对人体肝细胞LO2和小鼠乳腺癌细胞4T1无细胞毒性,而PDCL-PMPC/LDN胶束相比于裸药LDN对4T1细胞具有更好的抑制效果,呈现出更小的IC50。因此,合成的阳离子聚合物PDCL-PMPC胶束具有被用于抗癌药物载体的潜力。In this study,the amphipathy cationic copolymer containing phosphatidylcholine biomimetic structure,poly{α-[4-(diethylamino)methyl-1,2,3-triazol]-caprolactone-co-caprolactone}-b-poly(2-methacryloyloxyethyl phosphorylcholine)(PDCL-PMPC),was synthesized by click reaction and ATRP.The structure was confirmed by 1H-NMR,FT-IR and DSC.The results of DLS and SEM show that the PDCL-PMPC can self-assemble into spherical micelles with the particle size of 120 nm in water.It is found that the micelles have a high loading capacity for superhydrophobic anionic drug LDN.MTT assay in vitro indicates that the blank PDCL-PMPC micelles have no cytotoxicity to human hepatocyte LO2 and mouse breast cancer cell 4T1,while the LDN encapsulated in PDCL-PMPC micelles has better inhibitory effect on 4T1 cells than free drug,showing a lower IC50.Therefore,the synthesized cationic polymer PDCL-PMPC has potential as an anticancer drug carrier.

关 键 词：磷脂胆碱 阳离子聚合物 氯尼达明 药物载体 

分 类 号：TQ460.1[化学工程—制药化工]