pH- and redox-responsive self-assembly of amphiphilic hyperbranched poly(amido amine)s for controlled doxorubicin delivery.
pH- and redox-responsive self-assembly of amphiphilic hyperbranched poly(amido amine)s for controlled doxorubicin delivery.
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DOI：
10.1039/c4bm00410h
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发表时间：
2015-03
影响因子：
6.6
通讯作者：
Wei‐Xing Cheng;J. Kumar;Yong Zhang;Ye Liu
中科院分区：
文献类型：
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作者：
Wei‐Xing Cheng;J. Kumar;Yong Zhang;Ye Liu
乙烯基封端的超支化聚（酰胺基胺）是通过 4-（氨基甲基）哌啶（AMPD）与双摩尔 N,N-胱胺双（丙烯酰胺）（BAC）进行迈克尔加成聚合而获得的。然后，通过将乙烯基转化为胺，然后进行聚乙二醇化，产生两亲性超支化聚(BAC2-AMPD1)-PEG。透射电子显微镜（TEM）、动态光散射（DLS）和（1）H核磁共振（NMR）结果表明，胶束可以通过超支化聚（BAC2-AMPD1）-PEG的自组装获得。此外，可以将抗癌药物阿霉素（DOX）装载到胶束中。研究了不含和含有 DOX 的超支化聚 (BAC2-AMPD1)-PEG 胶束的 pH 和氧化还原反应。共聚焦显微镜和流式细胞术结果表明，FITC标记或负载DOX的超支化聚(BAC2-AMPD1)-PEG胶束可以进入HepG2和MCF-7细胞，并且在细胞核中可以观察到DOX。在 HepG2 和 MCF-7 细胞中评估了不含和含有 DOX 的胶束的细胞毒性，并与游离 DOX 进行了比较，讨论了杀死癌细胞的功效。
Vinyl-terminated hyperbranched poly(amido amine)s is obtained by Michael addition polymerization of 4-(aminomethyl)piperidine (AMPD) with a double molar N,N-cystaminebis(acrylamide) (BAC). Then an amphiphilic hyperbranched poly(BAC2-AMPD1)-PEG is produced via converting the vinyl groups to amines followed by PEGylation. Transmission electron microscopy (TEM), dynamic light scattering (DLS), and (1)H nuclear magnetic resonance (NMR) results indicate that the micelles can be obtained via self-assembly of hyperbranched poly(BAC2-AMPD1)-PEG. Further an anti-cancer drug, doxorubicin (DOX), can be loaded into the micelles. pH- and redox-response of the micelles of hyperbranched poly(BAC2-AMPD1)-PEG without and with DOX are investigated. The results of confocal microscopy and flow cytometry reflect that FITC tagged or DOX loaded micelles of hyperbranched poly(BAC2-AMPD1)-PEG can enter HepG2 and MCF-7 cells, and DOX can be observed in the nucleus of the cells. The cytotoxicity of the micelles without and with DOX is evaluated in HepG2 and MCF-7 cells, and the efficacy to kill the cancer cells is discussed in comparison with free DOX.