交联星型聚合物胶束的制备及其抗肿瘤应用  

Preparation of Crosslinked Star Polymer Micelles and Their Antitumor Applications

作　　者：赵健清 唐昭敏 ZHAO Jianqing;TANG Zhaomin(School of New Energy and Materials,Southwest Petroleum University,Chengdu 610500,China)

机构地区：[1]西南石油大学新能源与材料学院,四川成都610500

出　　处：《工业微生物》2023年第4期10-12,共3页Industrial Microbiology

摘　　要：传统聚合物胶束因稳定性不足容易在血液循环的剪切力及蛋白质的作用下解体,导致封装的化疗药物提前释放,使得药物在体内进行非特异性分布并产生了毒副作用。为解决该问题,文章合成了基于聚赖氨酸的两亲性三嵌段共聚物m PEG-P(LL/LL-LA)-PCL,通过溶剂蒸发法制备非交联胶束DUCM,再利用二硫苏糖醇DTT诱导赖氨酸LA发生交联,在亲疏水壳层之间形成了还原响应型交联网络结构从而制备得到交联胶束DCM。基于内部的交联结构,DCM可以在血液循环中保持稳定,进入肿瘤细胞后,还原响应型交联网络结构中的二硫键会在肿瘤细胞中高表达的谷胱甘肽(GSH)的作用下断裂从而释放化疗药物,达到杀死肿瘤细胞的目的。文章通过合理的结构设计,提高了PEG-PCL胶束的稳定性及刺激响应性,为其他胶束药物传递系统的研发提供了参考。Traditional polymer micelles are prone to disintegration under the shear force of blood circulation and protein action due to insufficient stability,leading to early release of encapsulated chemotherapy drugs,causing non-specific distribution of drugs in the body and producing toxic side effects.In order to solve this problem,an amphiphilic triblock copolymer mPEG-P(LL/LL-LA)-PCL based on polylysine was synthesized in the paper.Non crosslinked micelles DUCM were prepared by solvent evaporation method,and then cross-linked lysine LA was induced by dithiothreitol DTT to form a reductive responsive cross-linking network structure between hydrophilic and hydrophobic water shells to obtain crosslinked micelles DCM.Due to its internal cross-linking structure,DCM can maintain stability in the blood circulation.After entering tumor cells,the disulfide bonds in the reductive responsive cross-linking network structure will break under the action of highly expressed glutathione(GSH)in tumor cells,releasing chemotherapy drugs and achieving the goal of killing tumor cells.The paper improves the stability and stimulation response of PEG-PCL micelles through reasonable structural design,providing a reference for the development of other micellar drug delivery systems.

关 键 词：交联胶束 化疗 刺激响应 

分 类 号：TQ460.4[化学工程—制药化工] TQ317