Dj. Begley, THE BLOOD-BRAIN-BARRIER - PRINCIPLES FOR TARGETING PEPTIDES AND DRUGSTO THE CENTRAL-NERVOUS-SYSTEM, Journal of Pharmacy and Pharmacology, 48(2), 1996, pp. 136-146
The presence of the blood-brain barrier (BBB), reduces the brain uptak
e of many drugs, peptides and other solutes from blood. Strategies for
increasing the uptake of drugs and peptide-based drugs include; struc
tural modifications to increase plasma half-life; improving passive pe
netration of the BBB by increasing the lipophilicity of the molecule;
designing drugs which react with transporters present in the BBB; and
reducing turnover and efflux from the central nervous system (CNS).