共价键
前药
化学
药品
结合
聚合物
组合化学
药理学
生物物理学
有机化学
生物化学
医学
数学
生物
数学分析
作者
Panagiotis Theodosis-Nobelos,Despina Charalambous,Charalampos Triantis,Maria Rikkou-Kalourkoti
出处
期刊:Current Drug Delivery
[Bentham Science]
日期:2020-09-15
卷期号:17 (7): 542-557
被引量:10
标识
DOI:10.2174/1567201817999200508092141
摘要
Polymer-drug conjugates are polymers with drug molecules chemically attached to polymer side chains through either a weak (degradable bond) or a dynamic covalent bond. These systems are known as pro-drugs in the inactive form when passing into the blood circulation system. When the prodrug reaches the target organ, tissue or cell, the drug is activated by cleavage of the bond between the drug and polymer, under certain conditions existing in the target organ. The advantages of polymer-drug conjugates compared to other controlled-release carriers and conventional pharmaceutical formulations are the increased drug loading capacity, prolonged <i>in vivo</i> circulation time, enhanced intercellular uptake, better-controlled release, improved therapeutic efficacy, and enhanced permeability and retention effect. The aim of the present review is the investigation of polymer-drug conjugates bearing anti-cancer drugs. The polymer, through its side chains, is linked to the anti-cancer drugs <i>via</i> dynamic covalent bonds, such as hydrazone/imine bonds, disulfide bonds, and boronate esters. These dynamic covalent bonds are cleaved in conditions existing only in cancer cells and not in healthy ones. Thus, ensuring the selective release of drug to the targeted tissue, reducing in this way, the frequent side effects of chemotherapy, leading to a more targeted application, despite the nature of the applied polymer, possessing the ability to aim tumors selectively <i>via</i> incorporation of a relative ligand.
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