Polymer micelles with cross-linked polyanion core for delivery of a cationic drug doxorubicin.
Polymer micelles with cross-linked polyanion core for delivery of a cationic drug doxorubicin.
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DOI：
10.1016/j.jconrel.2009.04.019
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发表时间：
2009-09-15
影响因子：
10.8
通讯作者：
Bronich, Tatiana K.
中科院分区：
文献类型：
--
作者：
Kim, Jong Oh;Kabanov, Alexander V.;Bronich, Tatiana K.
以聚氧化乙烯-b-聚甲基丙烯酸共聚物（PEO-b-PMA）嵌段离聚物和二价金属离子为模板，制备了具有交联离子核的聚合物胶束。阿霉素（DOX），蒽环类抗癌药物，成功地纳入到这样的胶束的离子核心通过静电相互作用。实现了大量的载药水平（高达50 w/w %），它强烈依赖于交联胶束的结构和pH值。载药胶束在水性分散体中稳定，长时间内没有聚集或沉淀。由于胶束核中羧基的质子化作用，DOX在酸性环境中具有明显的pH敏感性，加速释放。用聚阳离子物质保护载药核的尝试导致载药效率降低，并对胶束的释放特性产生轻微影响。阿霉素聚合物胶束对人卵巢癌A2780细胞具有较强的细胞毒性。这些结果指出了具有交联离子核的新型聚合物胶束成为递送DOX的有吸引力的载体的潜力。
Polymer micelles with cross-linked ionic cores were prepared by using block ionomer complexes of poly(ethylene oxide)-b-poly(methacrylic acid) (PEO-b-PMA) copolymer and divalent metal cations as templates. Doxorubicin (DOX), an anthracycline anticancer drug, was successfully incorporated into the ionic cores of such micelles via electrostatic interactions. A substantial drug loading level (up to 50 w/w %) was achieved and it was strongly dependent on the structure of the cross-linked micelles and pH. The drug-loaded micelles were stable in aqueous dispersions exhibiting no aggregation or precipitation for a prolonged period of time. The DOX-loaded polymer micelles exhibited noticeable pH-sensitive behavior with accelerated release of DOX in acidic environment due to the protonation of carboxylic groups in the cores of the micelles. The attempt to protect the DOX-loaded core with the polycationic substances resulted in the decrease of loading efficacy and had a slight effect on the release characteristics of the micelles. The DOX-loaded polymer micelles exhibited a potent cytotoxicity against human A2780 ovarian carcinoma cells. These results point to a potential of novel polymer micelles with cross-linked ionic cores to be attractive carriers for the delivery of DOX.
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影响因子：
5.8
作者：
Alakhov, V;Klinski, E;Kabanov, A
通讯作者：
Kabanov, A
影响因子：
10.8
作者：
Oh, Kyung T.;Bronich, Tatiana K.;Kabanov, Alexander V.
通讯作者：
Kabanov, Alexander V.
影响因子：
5.5
作者：
Bronich, TK;Kabanov, AV;Eisenberg, A
通讯作者：
Eisenberg, A
影响因子：
3.8
作者：
HIGUCHI, T
通讯作者：
HIGUCHI, T
影响因子：
3.3
作者：
Kabanov, VA;Skobeleva, VB;Zezin, AB
通讯作者：
Zezin, AB