紫杉醇前药的研究概况

Progress in the Development of Paclitaxel prodrugs

目的综述了治疗肿瘤的一线药物,紫杉醇前药的研究进展。方法通过查阅近年来国内外的相关文献,选取有代表性的学术期刊,专利进行分析评述。结果利用前药原理设计的小分子前药,高分子聚合物前药,大分子前药等改善了紫杉醇的应用状况。这些前药通过体内特异性的酶或PH值降解释放出原药。结论前药增大了紫杉醇的水溶性,可以达到靶向、控释、缓释的效果,降低毒副作用,提高了抗肿瘤活性,并且很多前药已经进入临床研究阶段。

OBJECTIVE To review the development of paclitaxel（TAX）prodrug,which has a significant role as a first-line drug in the treatment of various tumors.METHODS This review paper referred to literature at home and abroad in recent years,analyzed and induced the representative academic journals and patents.RESULTS Much progress has been made in the research of prodrug,such as low molecular,polymer,macromolecular,and so on.In vivo,Tax is removed from the prodrug via cleavage by enzyme or pH,which is specifically expressed in tumor tissues.CONCLUSION Prodrug as a cancer therapeutics drug obviously improves the hydrosoluble of TAX,enhances the efficacy of tumor-targeting,controlled release,sustained release and reduces the side effects compared with the original drug.Many prodrugs have entered into the stage of clinical evaluation.