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首页> 外文期刊>Journal of Applied Polymer Science >pH-sensitive hydroxyethyl starch-doxorubicin conjugates as antitumor prodrugs with enhanced anticancer efficacy
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pH-sensitive hydroxyethyl starch-doxorubicin conjugates as antitumor prodrugs with enhanced anticancer efficacy

机译：pH敏感的羟乙基淀粉-阿霉素缀合物作为抗肿瘤前药，具有增强的抗癌功效

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Doxorubicin (DOX) is a widely used chemotherapeutic drug for the treatment of several types of cancers, which has limitation in clinical applications because of severe heart toxicity. Herein, to reduce the fast clearance from the blood system and the severe systemic toxicity caused by the nonspecific protein adsorption, a pH-sensitive drug delivery system with higher drug conjugated content was prepared by conjugating DOX onto hydroxyethyl starch (HES) with a pH-sensitive hydrazone bond. In normal physiological environment, the release of DOX conjugated onto HES was slight which could be neglected without any side effect. However, in an acidic environment mimicking the tumor microenvironment, this pH-sensitive hydrazone linkage provided a controlled and sustained release of DOX over a period of more than 3 days. The conjugates had good biocompatibility, long circulation, and lower cytotoxicity, which could efficiently be transferred into HeLa and HepG2 cells and release the conjugated drug. Based on these promising properties, these HES-DOX conjugates outline the significant potential for future biomedical application in the controlled release of antitumor drugs. (c) 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 42778.
机译：阿霉素（DOX）是一种用于治疗多种类型癌症的广泛使用的化学治疗药物，由于严重的心脏毒性，其在临床应用中受到限制。在此，为了减少血液系统的快速清除和非特异性蛋白质吸附所引起的严重的全身毒性，通过将DOX与pH-敏感的bond键。在正常的生理环境中，缀合到HES上的DOX的释放很小，可以忽略不计，没有任何副作用。但是，在模拟肿瘤微环境的酸性环境中，这种对pH敏感的键可在超过3天的时间内提供受控且持续的DOX释放。该缀合物具有良好的生物相容性，长循环性和较低的细胞毒性，可以有效地转移到HeLa和HepG2细胞中并释放出缀合的药物。基于这些有前途的特性，这些HES-DOX共轭物概述了抗肿瘤药物控释中未来生物医学应用的巨大潜力。 （c）2015 Wiley Periodicals，Inc. J. Appl。 Polym。科学2015，132，42778。

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