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The use of polymeric platinum(IV) prodrugs to deliver multinuclear platinum(II) drugs with reduced systemic toxicity and enhanced antitumor efficacy

机译:聚合铂(IV)前药用于递送具有降低的全身毒性和增强的抗肿瘤功效的多核铂(II)药物

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摘要

Two dinuclear platinum(IV) prodrugs were prepared from cisplatin and oxaliplatin, and tethered to amphiphilic biodegradable block copolymers. The polymeric dinuclear platinum(IV) prodrugs were allowed to self-assemble into nanomicelles, which showed reduced systemic toxicity, relatively long blood circulation, and enhanced antitumor efficacy. In this way, the bottleneck of present multinuclear platinum drugs, especially their severe systemic toxicity, might be overcome.
机译:从顺铂和奥沙利铂制备了两种双核铂(IV)前药,并拴系到两亲性可生物降解的嵌段共聚物上。聚合的双核铂(IV)前药可以自组装成纳米胶束,从而显示出较低的全身毒性,相对长的血液循环和增强的抗肿瘤功效。这样,可以克服当前多核铂药物的瓶颈,特别是其严重的全身毒性。

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