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Review
. 1996 Feb;48(2):136-46.
doi: 10.1111/j.2042-7158.1996.tb07112.x.

The blood-brain barrier: principles for targeting peptides and drugs to the central nervous system

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Review

The blood-brain barrier: principles for targeting peptides and drugs to the central nervous system

D J Begley. J Pharm Pharmacol. 1996 Feb.

Abstract

The presence of the blood-brain barrier (BBB), reduces the brain uptake of many drugs, peptides and other solutes from blood. Strategies for increasing the uptake of drugs and peptide-based drugs include; structural modifications to increase plasma half-life; improving passive penetration 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).

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