Hilgenbrink Andrew R, Low Philip S
Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.
J Pharm Sci. 2005 Oct;94(10):2135-46. doi: 10.1002/jps.20457.
Folate targeted drug delivery has emerged as an alternative therapy for the treatment and imaging of many cancers and inflammatory diseases. Due to its small molecular size and high binding affinity for cell surface folate receptors (FR), folate conjugates have the ability to deliver a variety of molecular complexes to pathologic cells without causing harm to normal tissues. Complexes that have been successfully delivered to FR expressing cells, to date, include protein toxins, immune stimulants, chemotherapeutic agents, liposomes, nanoparticles, and imaging agents. This review will summarize the applications of folic acid as a targeting ligand and highlight the various methods being developed for delivery of therapeutic and imaging agents to FR-expressing cells.
叶酸靶向给药已成为治疗和成像多种癌症及炎症性疾病的一种替代疗法。由于其分子尺寸小且对细胞表面叶酸受体（FR）具有高结合亲和力，叶酸缀合物能够将多种分子复合物递送至病理细胞，而不会对正常组织造成损害。迄今为止，已成功递送至表达FR的细胞的复合物包括蛋白质毒素、免疫刺激剂、化疗药物、脂质体、纳米颗粒和成像剂。本综述将总结叶酸作为靶向配体的应用，并重点介绍为将治疗剂和成像剂递送至表达FR的细胞而正在开发的各种方法。
