【摘要】 喜树碱具有广谱抗癌活性,但其水溶性差和毒副作用大等缺点限制了其在临床上的使用。为使喜树碱类药物能够更好地应用于临床,除了喜树碱的结构修饰和改造,新型药物传递系统的应用使喜树碱的功能得以更好地发挥,亦成为研究热点之一。文章总结近年来喜树碱传递系统及功能发挥的研究进展,在增加药物水溶性、提高内酯环稳定性以及药物控释与靶向传递几个方面进行了文献综述。随着相关技术的不断完善和发展,喜树碱类药物将是极具发展前景的一类抗癌药物。更多还原

【Abstract】 Camptothecin is known to possess a broad spectrum of anticancer activities, however due to its high toxicity and low solubility in water, camptothecin is severely limited in clinic. To optimize the effects of camptothecin in the treatment of malignancies, besides the structural modification and reconstruction of camptothecin, the establishment of new drug delivery systems becomes a hot topic in the camptothecin research. This paper aims to summarize the advanced progress in the delivery system and function of camptothecin at recent years. The advances in improving the poor solubility, lactone ring instability, controlled release systems and targeting delivery systems of camptothecin are also reviewed. As the related methods and technologies are improved and developed, camptothecin will be a group of prospective anticancer drugs.更多还原