Nanomedicine from amphiphilizedprodrugs: concept and clinical translation.
Nanomedicine from amphiphilizedprodrugs: concept and clinical translation.
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DOI：
10.1016/j.addr.2021.114027
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发表时间：
2021-10
影响因子：
16.1
通讯作者：
Jiajia Xiang;Xin Liu;Guiping Yuan;Runnan Zhang;Zhou Quan;Tao Xie;Youqing Shen
中科院分区：
文献类型：
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作者：
Jiajia Xiang;Xin Liu;Guiping Yuan;Runnan Zhang;Zhou Quan;Tao Xie;Youqing Shen
纳米药物通常由载体材料和少量活性药物成分(API)组成，长期以来一直被用于改善药物动力学和生物分布，增强治疗效果和减轻副作用。由于两亲化前药策略具有许多优点，包括使用最少的惰性载体材料、表征良好的前药结构、固定和高载药量、100%的载药效率、以及无突发性但可控的药物释放，因此将疏水/亲水药物两亲化为能够自组装成明确的纳米结构的前药物已经成为一种简单的制备纳米药物的方法。本文综述了APDS及其纳米药物的最新研究进展，从按需药物释放的基本原理和刺激反应连接体化学到APDS的临床应用进展，APDS的临床表现，以及未来发展的挑战和展望。
Nanomedicines generally consisting of carrier materials with small fractions of active pharmaceutical ingredients (API) have long been used to improve the pharmacokinetics and biodistributions, augment the therapeutic efficacies and mitigate the side effects. Amphiphilizing hydrophobic/hydrophilic drugs to prodrugs capable of self-assembly into well-defined nanostructures has emerged as a facile approach to fabricating nanomedicines because this amphiphilized prodrug (APD) strategy presents many advantages, including minimized use of inert carrier materials, well-characterized prodrug structures, fixed and high drug loading contents, 100% loading efficiency, and burst-free but controlled drug release. This review comprehensively summarizes recent advances in APDs and their nanomedicines, from the rationale and the stimuli-responsive linker chemistry for on-demand drug release to their progress to the clinics, clinical performance of APDs, as well as the challenges and perspective on future development.