[Non-invasive drug delivery system with the claudin binder]

The intercellular spaces between adjacent epithelial cells are sealed by tight junctions (TJs). Modulation of TJ-seal is a potent strategy for drug absorption. Claudin is a key structural and functional component of TJ-seal. Claudin comprises a tetra-transmembrane protein family consisting of more than 20 members, whose expression profiles and barrier-function differ among tissues. For instance, claudin-1 plays roles in the epidermal and mucosal barriers, and claudin-4 regulates the mucosal barrier. Claudin forms homo- and hetero-type TJ strands. Properties of TJ-seal are determined by combination of the claudin family members. Some claudin strands work as size-selective or charge-selective paracellular routes for solutes. Thus, claudin modulators will make it possible to deliver drugs in a solute- and tissue-specific manner. The C-terminal fragment of the Clostridium perfringens enterotoxin (C-CPE) is the most characterized claudin modulator. In this review, we describe potency of claudin-targeting mucosal absorption, and we mentioned development of a novel claudin modulator using C-CPE as a prototype.