ABSTRACT
Drug delivery systems using polymers as drug carriers have been investigated to achieve the efficient delivery of anticancer agents to tumor cells. In comparison with a low molecular-weight prodrug, a macromolecular prodrug is expected to overcome the problem of side effects by improving drug distribution in the body and prolongation of its activity. Cis-dichlorodiammineplatinum (II) (cisplatin, CDDP) has been widely used for clinical cancer therapy in spite of its severe renal toxicity and low water-solubility. The chapter provides a macromolecular prodrug of CDDP that has reduced side-effects and good water solubility, aims to design CDDP polymer/dextran derivatives complexes with carboxylic acid groups, oxidized dextran (OX-Dex)/CDDP conjugates, and dicarboxymethyl dextran (DCM-Dex)/CDDP conjugates. The pharmacokinetics of free CDDP, OX-Dex/CDDP, and DCM-Dex/CDDP conjugates after intravenous injection in rat and their growth inhibitory effects against colon 26 tumor bearing mice by intravenous injection were investigated.
