叶酸受体介导靶向给药系统研究进展

Advances in research on folate receptor-mediated targeted delivery systems

靶向给药系统是诊断和治疗癌症的一种有效方法,因其副作用小、治疗效果好而受到广泛关注。叶酸受体在多数癌细胞表面过度表达,但在正常细胞表面低表达或未表达,与配体叶酸具有高度的亲和力。叶酸连接到药物载体上,可靶向作用于癌细胞。介绍了叶酸与叶酸受体,简述了叶酸受体介导靶向的作用机制,讨论了叶酸连接脂质体、胶束、纳米粒、聚合物载体、液晶叶酸纳米粒、负载药物通过叶酸受体介导诊治癌症的研究进展,分析了各自的优点和不足,提出了叶酸受体介导靶向给药系统的未来研究方向一是对叶酸受体介导作用机制进行深入研究;二是对药物释放后载体的体内分布、代谢、排泄等过程做进一步探索;三是研究单一、易合成但高效的诊断或治疗剂,减少材料浪费,简化给药方式。

Targeted drug delivery system is an effective way to diagnose and treat cancer.Because of its small side effects and good therapeutic effect,it has been widely concerned.Folate receptor is over expressed on the surface of most cancer cells,but it is low or not expressed on the surface of normal cells.Folate has a high affinity with the ligand folate.Connected to the drug carrier,folate can target cancer cells.Folic acid and folic acid receptors were introduced,the mechanism of folate receptor mediated targeting was briefly described.Furthermore,the research progress of diagnosis and treatment of cancer by using folic acid linked liposomes,micelles,nanoparticles,polymer carriers,liquid crystalline folic acid nanoparticles and loaded drugs through folate receptor-mediated was discussed,and the advantages and disadvantages were analyzed.Finally,the prospect of folic acid receptor-mediated targeted drug delivery system was presented.The first is to study the mechanism of folic acid receptor mediated action deeply.The second is to further explore the distribution,metabolism,excretion and other processes of carriers after drug release.The third is to study a single,easily synthesized but highly effective diagnostic or therapeutic agent to reduce material waste and simplify administration methods.