两亲性透明质酸衍生物的合成及其在抗肿瘤纳米药物递送系统中的应用  

Preparation of Amphiphilic Hyaluronic Acid Derivatives and Their Applications in Anti-tumor Nano-drug Delivery Systems

作　　者：胡乐坚 刘富垒[1] 李凌超[1] 冯锋[1] 曲玮[1] 

机构地区：[1]中国药科大学天然药物化学教研室生物功能材料重点实验室,江苏南京211198

出　　处：《药学进展》2017年第11期804-811,共8页Progress in Pharmaceutical Sciences

基　　金：中国药科大学大学生创新创业训练计划项目(No.201610316121)

摘　　要：两亲性透明质酸衍生物装载药物形成载药纳米材料,可提高药物水溶性,增加药物稳定性,延长药物在血液中的循环时间,增强药物疗效并降低全身副作用。更为重要的是,透明质酸为肿瘤细胞高表达的透明质酸受体的配体,以两亲性透明质酸衍生物制备的载药材料具备肿瘤部位主动靶向性和肿瘤细胞摄取促进能力,因此,其在纳米载药递送系统中具有良好的应用前景。综述两亲性透明质酸衍生物的合成方法及其在抗肿瘤纳米药物递送系统中的应用,并探究不同修饰形式的两亲性透明质酸衍生物与CD44受体的相互作用情况。Loading of drugs onto amphiphilic hyaluronic acid derivatives forms drug-loaded nano-materials. This system could increase watersolubility and chemical stability ofanticancer drugs, prolong blood circulation, enhance therapeutic efficiency and reduce side effects. More importantly, hyaluronic acid is the ligand of CD44 receptors highly expressed on tumor cells. Drug delivery systems based on amphiphilic hyaluronic acid derivatives can improve tumor targeting and internalization into tumor cells via CD44 receptor-mediated endocytosis, showing a promising application prospect. We reviewed the common chemical strategies for preparing hyaluronic acid derivatives their applications in anti-tumor nano-drug delivery systems, and the interaction between amphiphilic hyaluronic acid derivatives with different modifications and CD44 receptors.

关 键 词：透明质酸 结构修饰 纳米载药递送系统 CD44 

分 类 号：R943[医药卫生—药剂学]