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Preparation andIn VivoEvaluation of Dichloro(1,2-Diaminocyclohexane)platinum(II)-Loaded Core Cross-Linked Polymer Micelles

机译:负载二氯(1,2-二氨基环己烷)铂(II)的核交联聚合物胶束的制备和体内评价

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The therapeutic performance of oxaliplatin can be improved by incorporating the centralcis-dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt) motif into the core cross-linked block copolymer micelles. We describe here the preparation, cellular uptake, andin vivoevaluation of core cross-linked micelles loaded with DACHPt. Stable drug-loaded micelles were prepared at high drug loading (~25 w/w%) and displayed a considerably increasedin vitrocytotoxicity compared to free oxaliplatin against A2780 ovarian cancer cells. The DACHPt-loaded micelle formulation was well tolerated in mice and exhibited improved antitumor activity than oxaliplatin alone in an ovarian tumor xenograft model.
机译:通过将中心顺式-二氯(1,2-二氨基环己烷)铂(II)(DACHPt)基序并入核心交联的嵌段共聚物胶束中,可以提高奥沙利铂的治疗性能。我们在这里描述了载有DACHPt的核心交联胶束的制备,细胞摄取和体内评估。在高载药量(〜25%w / w%)下制备了稳定的载药胶束,与游离奥沙利铂相比,抗A2780卵巢癌细胞的体外细胞毒性显着提高。载有DACHPt的胶束制剂在小鼠中具有良好的耐受性,并且在卵巢肿瘤异种移植模型中比单独使用奥沙利铂具有更好的抗肿瘤活性。

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