Abstract Despite the fact that mitoxantrone (MTX) is an effective prescription drug for cancer therapy, its poor water solubility is a great challenge that limits its practical applications. Herein, to overcome this shortcoming, a drug/polymer conjugate of MTX with poly (ethyleneglycol) acrylate (PEG-A) (MTX/PPEG-A) was developed via in situ reversible addition-fragmentation chain transfer (RAFT) polymerization. Impressively, the MTX/PPEG-A conjugate shows highly improved water solubility, which is about 550% that of the unmodified MTX. The synthesized MTX/PPEG-A conjugate drug efficacy can be maintained and cytotoxicity reduced slightly compared with the unmodified MTX. In addition, the MTX/PPEG-A can be hydrolyzed by the esterase into pristine MTX with restored drug efficacy in vivo. All in all, the significant improvement of the water solubility and the slightly improved biocompatibility of MTX/PPEG-A will be well-suited for the administration and delivery of anti-cancer drugs in cancer therapy.

中文翻译：

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通过 RAFT 聚合将 PEG 丙烯酸酯原位接枝到具有脂肪族羟基官能团的药物上，以合成具有改善水溶性的药物/聚合物偶联物

摘要 尽管米托蒽醌（MTX）是一种有效的癌症治疗处方药，但其水溶性差是限制其实际应用的一大挑战。在此，为了克服这一缺点，通过原位可逆加成-断裂链转移 (RAFT) 聚合，开发了 MTX 与聚 (乙二醇) 丙烯酸酯 (PEG-A) (MTX/PPEG-A) 的药物/聚合物偶联物。令人印象深刻的是，MTX/PPEG-A 缀合物显示出高度改善的水溶性，约为未修饰 MTX 的 550%。与未修饰的 MTX 相比，合成的 MTX/PPEG-A 缀合物药物功效可以保持，细胞毒性略有降低。此外，MTX/PPEG-A 可以被酯酶水解成原始 MTX，在体内恢复药物功效。总而言之，