Xiang Jiajia, Liu Xin, Yuan Guiping, Zhang Runnan, Zhou Quan, Xie Tao, Shen Youqing
Zhejiang Key Laboratory of Smart BioMaterials and Center for Bionanoengineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou, Zhejiang 310027, China; Key Laboratory of Biomass Chemical Engineering of the Ministry of Education, College of Chemical and Biological Engineering, Hangzhou, Zhejiang University, Hangzhou 310027, China; ZJU-Hangzhou Global Scientific and Technological Innovation Center, Hangzhou, Zhejiang 311215, China.
Department of Orthopaedic Surgery, Sir Run Run Shaw Hospital, Medical College of Zhejiang University, Hangzhou, Zhejiang 310016, China.
Adv Drug Deliv Rev. 2021 Dec;179:114027. doi: 10.1016/j.addr.2021.114027. Epub 2021 Oct 31.
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.
长期以来，纳米药物通常由含有少量活性药物成分（API）的载体材料组成，用于改善药代动力学和生物分布，增强治疗效果并减轻副作用。将疏水性/亲水性药物两亲化为能够自组装成明确纳米结构的前药，已成为一种制备纳米药物的简便方法，因为这种两亲化前药（APD）策略具有许多优点，包括惰性载体材料的使用量最小化、前药结构特征明确、药物负载量固定且高、负载效率100%以及无突释但可控的药物释放。本综述全面总结了APD及其纳米药物的最新进展，从按需药物释放的原理和刺激响应连接化学到它们进入临床的进展、APD的临床性能，以及未来发展面临的挑战和前景。
