Efflux transport systems for drugs at the blood-brain barrier and blood-cerebrospinal fluid barrier (Part 1).
Penetration through the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB) is necessary if a drug is to achieve the required concentration for a desired pharmacological effect. Efflux transport systems at the BBB and BCSFB provide a protective barrier function by removing drugs from the brain or cerebrospinal fluid and transferring them to the systemic circulation, respectively; several transporters at the BBB and BCSFB have been identified. Efflux transport should be taken into consideration during drug development to improve brain penetration and to avoid drug-drug interactions involving these transporters and subsequent side effects.
Kusuhara
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Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, University of Tokyo, Tokyo, Japan
Sugiyama
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Y