许多由高分子药物释放体系给药的药物,由于载药量不够、或者由于癌细胞的多药耐药性导致药物外排等种种原因,不能以有效的药物浓度作用于目的器官,从而导致治疗效果不理想。人们已经尝试以不同方式添加聚乙二醇1000维生素E琥珀酸酯(D-α-tocopheryl polyethylene glycol 1000 succinate,TPGS)来改良高分子药物释放体系中的各种不足。总结了近几年来各种添加TPGS的高分子药物释放体系的研究进展,对所有TPGS的添加情况进行了分类,从包埋率和载药量的测量,细胞检测以及动物实验等进行概述。以不同的方式添加TPGS均可大大提高高分子药物释放体系的载药量和包埋率,抑制多药耐药性,甚至使抗癌药物达到口服的效果,可从多方面改善高分子释放体系给药的性能。
Many drugs administered via polymer drug delivery systems cannot achieve desirable results due to many factors such as the low drug loading efficiency or the multidrug resistance of cancer cells, which leads to drug efflux. In order to solve the problems, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was added to the polymeric drug carriers through different methods. Recent advances on polymeric drug delivery systems with the addition of TPGS and different adding methods of TPGS are summarized. Relevant methods are also introduced, including the measurement of loading efficiency and loading capacity, in vitro experiment and in vivo study. The addition of TPGS could improve the drug loading efficiency and loading capacity of polymer drug delivery system greatly, inhibit the multidrug resistance, or make it possible to administrate anticaneer drugs orally, thereby improve the performance of polymer drug delivery systems.