Department of Pharmacy, School of Health Sciences, Frederick University, Nicosia, Cyprus.
Curr Drug Deliv. 2020;17(7):542-557. doi: 10.2174/1567201817999200508092141.
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 in vivo; 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 via; 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 via; incorporation of a relative ligand.
聚合物-药物偶联物是通过弱(可降解键)或动态共价键将药物分子化学连接到聚合物侧链上的聚合物。这些系统在进入血液循环系统时处于无活性形式的前药。当前药到达靶器官、组织或细胞时,在靶器官中存在的某些条件下,通过药物和聚合物之间的键的裂解,药物被激活。与其他控制释放载体和常规药物制剂相比,聚合物-药物偶联物的优点是增加了药物载药量、延长了体内循环时间、增强了细胞间摄取、更好地控制了释放、提高了治疗效果、增强了渗透性和保留效果。本综述的目的是研究带有抗癌药物的聚合物-药物偶联物。聚合物通过其侧链,通过动态共价键(如腙/亚胺键、二硫键和硼酸酯)与抗癌药物连接。这些动态共价键仅在癌细胞中而不是在健康细胞中被裂解。因此,确保药物选择性释放到靶向组织,从而减少化疗的频繁副作用,导致更有针对性的应用,尽管所应用的聚合物的性质通过相对配体的掺入具有选择性靶向肿瘤的能力。
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