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血-视网膜屏障(BRB)是眼部关键的生物学屏障,能够有选择性地调控外来物质进入眼内组织,因而也限制了药物从全身血液循环递送到眼后段的过程.目前,在人类基因组中已确定了两大转运载体超家族:溶质载体超家族和ATP结合盒超家族.随着对转运载体的表达及其功能作用进行深入的研究,转运载体在药物代谢动力学中的重要性逐渐显现.本文综述了氨基酸、寡肽、单羧酸、叶酸和核苷等转运载体,同时阐明了研究眼部转运载体对优化改进或研发以转运载体为靶向的药物递送系统,进一步提高药物在眼部的生物利用度,具有重要的现实意义.“,”Drug deliver to the posterior eye segment (retinal tissue and vitreous) via systemic administration is constrained due to the presence of blood-retinal barrier (BRB) ,which regulates the permeation of many substances from blood to retina selectively.Two major transporters have been identified in the human genome,and they are solute carrier superfamilies and ATP-binding cassette.As the function of transporters is being revealed,it has been clarifed that the transporters are very important in pharmacokinetics.This article reviewed the expression and functional activity of various BRB transporters, including amino acid, oligopeptide, monocarboxylate, folate, nucleoside transporters etc.,updated the current knowledge about the BRB transporters and elucidated the urgent need for the development of optimal and efficient drug delivery systems.Any approach to further improving the ocular bioavailability of drugs will be of significant clinical relevance.