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.