Block copolymer micelles, containing dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt), the oxaliplatin parent complex, were prepared through polymer-metal complex formation of DACHPt with poly(ethylene glycol)-poly(glutamic acid) block copolymer [PEG-P(Glu)] in distilled water. By dynamic light scattering (DLS) measurement, the micelle size was determined to be 40 nm with narrow distribution. The release of platinum complexes from the micelle core was measured in phosphate buffer saline (pH 7.4) at 37 degrees C. DACHPt-loaded micelle showed a sustained release rate of platinum after an induction period of 12 h. In the same conditions, the kinetic stability of DACHPt-loaded micelle was measured. The micelle was found to be very stable, keeping the initial size, for 240 h. Against murine colon adenocarcinoma 26 (C-26) cells, DACHPt-loaded micelle exhibited considerable in vitro cytotoxicity, lower than oxaliplatin but increasing with exposure time as a result of the release of platinum complexes from the micelle. In vivo biodistribution assay performed on tumor-bearing mice demonstrated that the micelle showed prolonged blood circulation due to its high stability and high tumor accumulation for a prolonged time.

中文翻译：

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负载二氯（1,2-二氨基环己烷）铂（II）（DACHPt）的聚合物胶束的制备和生物学特性。

通过与聚（乙二醇）-聚（谷氨酸）嵌段共聚物的聚合物-金属配合物形成DACHPt，制备了含有二氯（1,2-二氨基环己烷）铂（II）（DACHPt），草酸铂母体配合物的嵌段共聚物胶束。在蒸馏水中的[PEG-P（Glu）]。通过动态光散射（DLS）测量，确定胶束大小为40 nm，分布较窄。在磷酸盐缓冲液（pH 7.4）中，在37摄氏度下测量了铂络合物从胶束核心中的释放。DACHPt负载的胶束在诱导12小时后显示出铂的持续释放速率。在相同条件下，测量了加载DACHPt的胶束的动力学稳定性。发现该胶束非常稳定，可以保持初始大小240小时。针对鼠结肠腺癌26（C-2​​6）细胞，加载DACHPt的胶束在体外具有明显的细胞毒性，低于奥沙利铂，但由于从胶束中释放出铂络合物，其随暴露时间的延长而增加。在荷瘤小鼠身上进行的体内生物分布分析表明，由于胶束的高稳定性和长时间的高肿瘤蓄积性，胶束显示出延长的血液循环。