紫杉醇新剂型的研究进展

紫杉醇是一种广谱、高效的抗肿瘤药物,但由于其水溶性差,临床上应用的注射剂加入聚氧乙烯蓖麻油以增加紫杉醇的水溶性,但聚氧乙烯蓖麻油在体内会产生严重的毒副作用.为了解决紫杉醇注射剂中聚氧乙烯蓖麻油的毒性问题,开发紫杉醇新剂型是近年来新药研发的热点之一.该文综述了近年来研发的一些紫杉醇新剂型,如乳剂、胶束、环糊精包合物、脂质体、微球、纳米粒和药物释放支架等,并对其可行性进行了分析.

Progress in the development of novel pharmaceutical formulations of paclitaxel

Abstract：Paclitaxel （PTX） has a powerful antitumor effect against a wide spectrum of cancers. Clinically, PTX is administered to patients via i. v. infusion. Due to its low water solubility, PTX is currently solubilized in the presence of Cremophor EL. However, the use of Cremophor EL can induce severe side effects. To solve these side effects,great attention has been focused on the development of novel pharmaceutical formulations of paclitaxel with low toxicity in recent years. This paper reviewed some novel pharmaceutical formulations of paclitaxel, such as emulsions, micelles, cyclodextrin complex, liposome, microsphere, nanoparticles, drug release stents and so on. The feasibility of these novel pharmaceutical formulations was assessed.