靶向肿瘤微环境的紫杉醇前药研究进展

紫杉醇前药（paclitaxel prodrugs）的设计是一种提高药物制剂成药性、降低其毒副作用、增强抗肿瘤效果的有效手段。随着对前药研究的深入，利用肿瘤过表达的受体、酶、转运蛋白、谷胱甘肽及活性氧自由基以及肿瘤组织弱酸性及低氧环境等作为靶标进行的紫杉醇靶向性前药的研究已取得极大进展。综述近年来以肿瘤微环境特殊的病理与生理特征为靶标的紫杉醇前药的研究进展。

Research progress on tumor-targeting paclitaxel prodrugs

Paclitaxel is a natural compound with efficient broad-spectrum antitumor activity. However, the clinical application has been limited owing to the undesirable drawbacks, such as the poor water-solubility, cardiovascular toxicity and neurotoxicity. The design of paclitaxel prodrugs is an effective measure which can improve the drug''s druggability, alleviate its toxicity adverse effect and enhance its antitumor effect. With the in-depth research of prodrugs, tumor-targeting paclitaxel prodrugs which using the excessive receptors, specific enzymes, transporters, reactive oxide species, glutathione in tumor tissues as well as acidosis and hypoxia in tumors as specific targets, have made great progress. The relevant literature about paclitaxel prodrugs were reviewed in this paper, which targeted to the specific pathological and physiological features of tumor microenvironment in recent years.