叶酸偶联高分子抗肿瘤药物载体的研究及应用  

Antitumor drug carriers based on folate-conjugated polymers:investigation and application

作　　者：李琳[1] 牛卫宁[1] 李海亮[1] 尚晓娅[1] 钦传光[1,2] 

机构地区：[1]西北工业大学生命学院,西安710072 [2]西北工业大学理学院应用化学系,西安710129

出　　处：《国际药学研究杂志》2012年第5期396-401,共6页Journal of International Pharmaceutical Research

基　　金：国家自然科学基金(31001012;31101304);陕西省自然科学基础研究计划重点项目(2012JZ2002);西北工业大学研究生创业种子基金(Z2012198)

摘　　要：靶向治疗对肿瘤细胞的杀伤力强,不良反应少,在癌症治疗中发挥着重要作用。由于叶酸受体是高选择性的肿瘤标志物,其在许多肿瘤细胞表面均过度表达,通过叶酸受体介导的内吞作用将抗肿瘤药物靶向传递至肿瘤组织或细胞,提高了抗癌药物的治疗指数,目前叶酸受体靶向递药技术已受到广泛关注。而其中利用高分子为载体,偶联靶向配体叶酸和抗肿瘤药物形成的高分子偶联药物,能显著延长药物的半衰期,增加药物的稳定性和溶解性,降低药物的毒副作用,使叶酸高分子偶联药物具有良好的应用前景。本文就目前各类叶酸受体介导的高分子抗肿瘤药物进行综述。Targeted therapies for cancer have many advantages, such as strong harmful effects on tumor cell and low adverse effect. Due to the fact that the folate receptor is a highly selective tumor marker overexpressed on the surface of many cancer cells, an titumor agents are targetedly delivered to tumor tissues or cells via endocytosis mediated by folate receptor to improve the therapeutic ef ficiency. At present, the technology of folate receptor targeting drug delivery attracts extensive attention. Folatetargeted polymeranti tumor drug conjugates, which use polymer as the carrier coupling the targeting ligand folic acid and anticancer drugs, can significantly extend the drug halflife, increase drug stability and solubility, and reduce the side effects of drugs remarkably. All these characteris tics indicate that folic acid polymerdrug conjugates have a good application prospect. This review covers the various types of folate re ceptormediated polymeric antitumer drugs conjugates, with special emphasis on the more recent ones and their mechanism aspects.

关 键 词：叶酸受体 抗肿瘤药物 高分子药物载体 靶向递药 内吞作用 

分 类 号：TQ460.1[化学工程—制药化工] R943[医药卫生—药剂学]