Liposomal camptothecin with impproved lactone-moiety stability and enhanced antitumor activity

摘要

Camptothecin (CAM), a potent topoisomerase I inhibitor, has to date demonstrated only modest thereapeutic activity against human cancer. The drug contains a #delta#-lactone ring moiety which, at pH 7.4, hydrolyzes rapidly to yield a biologically inactive carboxylate form in human plasma. It is essential to protect the lactonering from converting to its inactive form in vivo.