基于糖基化修饰的靶向药物传递系统研究概况

Research Overview of Targeted Drug Delivery Systems Based on Glycosylation Modification

近年来,基于药物受体及转运体介导的靶向药物传递系统已被广泛研究,靶向药物传递系统增强药物在病变部位的浓度和疗效,最大限度地降低了药物毒副作用。人体不同细胞表面高表达的特异性凝集素受体及脑毛细血管内皮细胞、肿瘤细胞高表达的葡萄糖转运体亚型Ⅰ,可与其相应的糖基配体产生特异性识别。将糖基配体分子如甘露糖、半乳糖、葡萄糖等,键接在药物传递系统上,可赋予其靶向性。这些糖基配体具有无毒、无免疫原性、生物相容性和生物可降解性良好等诸多优点,可广泛用于对药物传递系统的糖基化修饰。本文综述了近5年来糖基化修饰药物传递系统的靶向机制、合成方法及靶向特性,并对其发展前景作了展望。

In recent years,targeted drug delivery system based on drug receptors and transporters has been extensively studied. Targeted drug delivery system could enhance the concentration and efficacy of drugs in the lesion site,also could minimize the side effects of drugs. The specific membrane lectin receptors of a number of cells, glucose transporter I located at the brain microvascular endothelial cells and cancer cells could be specifically recognized by its corresponding glycosyl ligands. Drug delivery system which was glycosylated modified with mannose,galactose or glucose ligands has gained targeting properties. These glycosyl ligands exhibiting nontoxicity,biodegradability and biocompatibility, have been widely used in the glycosylated modification of drug delivery system. The targeting mechanisms,synthesis methods and their targeted ability of glycosylated modified drug delivery systems are summarized,and also a brief prospect is given in this review.