ABSTRACT
Tumor cell selective targeting is an attractive approach to enhance the efficacy and therapeutic index of anticancer drugs. Targeted liposomal delivery is accomplished by attaching to the surface of drug-carrying liposomes a tumor cell-specific ligand via a lipophilic anchor. Folate receptor (FR) has been identified as a broad-spectrum tumor cell-surface marker. Lipophilic derivatives of folate, a high-affinity ligand for the FR, can be incorporated into liposomes for targeting tumor cells with amplified FR expression. This chapter will provide a brief overview of recent progress on FR-targeted liposomes, possible mechanisms for in vivo tumor targeting, and future directions.
