Centre for Advanced Macromolecular Design, (CAMD), The University of New South Wales, Sydney NSW 2052, Australia.
Chem Commun (Camb). 2013 Mar 14;49(21):2082-102. doi: 10.1039/c2cc36589h.
Polymers that start degrading under acidic conditions are increasingly investigated as a pathway to trigger the release of drugs once the drug carrier reached the slightly acidic tumour environment or after the drug carrier has been taken up by cells, resulting in the localization of the polymer in the acidic endosomes and lysosomes. The advances in the design of acid-degradable polymers and drug delivery systems have been summarized and discussed in this review article. Various acid-labile groups such as acetals, orthoester, hydrazones, imines and cis-aconityl, that can undergo cleavage in slightly acidic conditions, have been employed to create polymer architectures or polymer-drug conjugates that can degrade under lysosomal and endosomal conditions, triggering the fast release of drugs or DNA.
聚合物在酸性条件下开始降解，这一特性被越来越多地研究作为一种途径，以触发药物释放，一旦药物载体到达微酸性肿瘤环境，或者在药物载体被细胞摄取后，导致聚合物在酸性内涵体和溶酶体中定位。本文综述并讨论了酸降解聚合物和药物传递系统的设计进展。各种酸不稳定基团，如缩醛、原酸酯、腙、亚胺和顺式丙烯酰，在微酸性条件下可以发生断裂，已被用于构建聚合物结构或聚合物-药物偶联物，这些聚合物在溶酶体和内涵体条件下可以降解，从而快速释放药物或 DNA。
