Hatefi A, Amsden B
Faculty of Pharmacy, University of Alberta, Edmonton, Canada.
Pharm Res. 2002 Oct;19(10):1389-99. doi: 10.1023/a:1020427227285.
Camptothecin has shown significant antitumor activity to lung, ovarian, breast, pancreas, and stomach cancers. Camptothecin, however, like a number of other potent anticancer agents such as paclitaxel, is extremely water insoluble. Furthermore, pharmacology studies have determined that prolonged schedules of administration given continuously are required. Thus, this insolubility has restricted its clinical application. For these reasons, a number of water-soluble analogs have been synthesized and a number of different formulation approaches have been investigated. In this review, we examine each of these approaches and discuss their advantages and limitations.
喜树碱已显示出对肺癌、卵巢癌、乳腺癌、胰腺癌和胃癌具有显著的抗肿瘤活性。然而，喜树碱与许多其他强效抗癌药物如紫杉醇一样，极难溶于水。此外，药理学研究已确定需要持续长时间给药。因此，这种不溶性限制了其临床应用。出于这些原因，人们合成了许多水溶性类似物，并研究了许多不同的制剂方法。在本综述中，我们研究了这些方法中的每一种，并讨论了它们的优点和局限性。
