This review focuses on epithelial drug transport mechanisms in mucosal drug delivery: the final step of a four-part process. Reference is made to the mucosae lining the oral cavity and the gastrointestinal tract, the two mucosae most often succumbing to the side effects of cytotoxic chemotherapeutic drugs. This review will be devoted to carrier-mediated transport, particularly as it relates to the intestinal dipeptide transporter PepT1. This transporter protein appears to be enriched in tumor epithelial cells, to be rather robust to the cytotoxic effects of chemotherapeutic drugs, and to lend itself to the molecular engineering of drugs that target this transporter in tumor epithelial cells. In contrast to the gastrointestinal tract, much less is known about the type and capacity of drug transport processes in the buccal epithelial cells and about how these processes may be altered in disease state (including cancer) and be manipulated pharmaceutically to optimize drug absorption.