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该文合成了一种具有pH敏感性,较低毒性的两亲性嵌段共聚物以用于药物运输。聚乙二醇-聚己内酯(mPEG-PCL)是以聚乙二醇单甲醚为引发剂,开环己内酯聚合而成,阿霉素则是通过顺乌头酸裂解键连在聚己内酯的末端。该嵌段聚合物通过核磁共振、红外光谱等进行表征。共轭阿霉素后的嵌段聚合物在水溶液中能够自组装形成胶束,胶束粒径约为45.4 nm,透射电镜显示胶束具有近似的球形结构。阿霉素在pH=4.0下的释放速率明显快于pH=7.4下的释放速率。mPEG-PCL在细胞培养中无细胞毒性,包载阿霉素的胶束在人类MCF-7乳腺癌细胞上表现出迟缓的细胞毒性。通过共聚焦显微镜观察游离阿霉素和mPEG-PCL-DOX胶束在MCF-7细胞内的定位说明载体能够携带阿霉素进入细胞。
This paper synthesized a pH-sensitive, less toxic amphiphilic block copolymer for drug delivery. Polyethylene glycol-polycaprolactone (mPEG-PCL) is polyethylene glycol monomethyl ether as initiator, open-loop caprolactone polymerization from doxorubicin is cleaved by cis-aconitic acid linkage The end of polycaprolactone. The block polymer is characterized by nuclear magnetic resonance, infrared spectroscopy and the like. The conjugate doxorubicin block polymer can self-assemble into micelles in aqueous solution. The size of the micelles is about 45.4 nm. Transmission electron microscopy shows that the micelles have an approximately spherical structure. The rate of doxorubicin release at pH = 4.0 was significantly faster than at pH = 7.4. mPEG-PCL is non-cytotoxic in cell culture and doxorubicin-loaded micelles exhibit delayed cytotoxicity on human MCF-7 breast cancer cells. The localization of free doxorubicin and mPEG-PCL-DOX micelles in MCF-7 cells by confocal microscopy showed that the vector could carry doxorubicin into the cells.