BLOOD-BRAIN BARRIER DRUG TARGETING: THE FUTURE OF BRAIN DRUG DEVELOPMENT

Outline of a program for developing BBB drug targeting strategies derived from either chemistry-based or biology-based disciplines. Chemistry-based strategies emphasize lipid solubility, hydrogen bonding, and molecular weight of the drug. Biology-based strategies emphasize endogenous BBB transporters. Small molecules can be transported across the BBB by either accessing certain carrier-mediated transport (CMT) systems or by inhibiting certain active efflux transporters (AET). Large-molecule drugs such as recombinant proteins or gene medicines can be delivered across the BBB via the receptor-mediated transport (RMT) systems. Reprinted with permission (11).