In the last decades, nanoscale drug delivery systems have gained great attention partly due to their ability to improve the bioavailability of water insoluble drugs. To this end, the general aim in developing nanomedicine is to enhance efficacy, drug stability and drug safety profile ideally by an active- or passive-cell specific targeting effect. Alteration of dose-response and potential personalization might be future trademarks of nanomedicine. Macromolecular prodrugs (MPDs) represent a sub-class of polymer-drug conjugates featuring a degradable linkage between a macromolecule and a drug. MPDs are in particular interesting due to their capability to prolong blood circulation and to reduce side effects caused by minimized premature drug leakage. The maximum drug loading capacity is another advantage of MPDs over conventional nanomedicines. The chemical accessibility of drug conjugates and polymer carrier materials as well as recent developments in the MPD design of the last five years are summarized in this review article.

中文翻译：

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大分子前药合成方法的最新进展


在过去的几十年中，纳米级药物递送系统受到了极大的关注，部分原因是它们能够提高水不溶性药物的生物利用度。为此，开发纳米医学的总体目标是通过主动或被动细胞特异性靶向作用来增强疗效、药物稳定性和药物安全性。剂量反应的改变和潜在的个性化可能是纳米医学未来的标志。大分子前药 (MPD) 代表聚合物-药物缀合物的一个子类，其特征是大分子和药物之间具有可降解的连接。 MPD 特别令人感兴趣，因为它们能够延长血液循环并减少因药物过早泄漏而引起的副作用。最大载药量是 MPD 相对于传统纳米药物的另一个优势。这篇综述文章总结了药物缀合物和聚合物载体材料的化学可及性以及过去五年 MPD 设计的最新进展。