叶酸修饰聚合物和脂质体药物载体及其靶向治疗的研究现状*

背景：叶酸介导的靶向药物载体被广泛研究。 目的：总结叶酸修饰靶向聚合物和脂质体药物载体的研究现状。 方法：由作者应用计算机检索2000-01/2010-12 Web of Science和CNKI数据库，选择叶酸修饰靶向聚合物和脂质体药物载体的相关文章，英文检索词为“folic acid, drug carriers, targeted delivery system, polymer, liposome”，中文检索词为“叶酸，药物载体，靶向，聚合物，脂质体”。共纳入相关文献19 篇进行综述。 结果与结论：叶酸受体在多种肿瘤细胞表面过度表达，而在多数正常组织中的表达仅限于一些难于进入血液循环的上皮细胞顶膜。正因为叶酸受体表达的特性，叶酸受体天然配体——叶酸成为将药物靶向到肿瘤细胞的重要分子。叶酸具有与叶酸受体的高亲和力、低免疫原性等优点，这使得叶酸介导肿瘤靶向的研究得到迅速发展。含叶酸靶向的药物载体体系中，主要分为3大类：即人工合成高分子载体体系、脂质体和天然高分子载体体系。 

Research status of folate-conjugated polymer and liposome as targeted drug carriers

BACKGROUND: Targeted drug carriers mediated by folic acid are studied widely. OBJECTIVE: To summarize the research status of folate-conjuated polymers and liposomes as targeted drug carriers. METHODS: The first author searched Web of Science and CNKI for articles (2000-01/2010-12) concerning the folate-conjuated polymers and liposomes as targeted drug carriers with the key words of “folic acid, drug carriers, targeted delivery system, polymer, liposome” in English and “folic acid, drug carriers, targeted, polymer, liposome” in Chinese. Nineteen articles were selected to review. RESULTS AND CONCLUSION: Folate receptor could overexpressed on the surface of many tumor cells, but the overexpression of folate receptor in the normal tissues is limited to apical membrane of epithelial cells which are difficult to enter the blood circulation. Because of the characteristics of folate receptor expression, natural ligands of folate receptor-folic acid are considered as an important molecule in transfer targeted drugs to tumor cells. Folic acid has the advantages of high affinity and low immunogenicity with folate receptor. Thus researches on folic acid-mediated targeted delivery systems are developed promptly. There are mainly three kinds of folate-modified drug carriers: synthesized polymers, liposomes and natural macromolecules.