Assessment of Blood-Brain Barrier Penetration: In Silico, In Vitro and In Vivo

Author(s): Meihua Rose Feng.

Journal Name: Current Drug Metabolism

Volume 3 , Issue 6 , 2002


The amount of drug achieved and maintained in the brain after systemic administration is determined by the agents permeability at blood-brain barrier (BBB), potential involvement of transport systems, and the distribution, metabolism and elimination properties. Passive diffusion permeability may be predicted by an in silico method based on a molecules structure property. In vitro cell culture is another useful tool for the assessment of passive permeability and BBB transports (e.g. PGP, MRP). In situ or in vivo techniques like carotid artery single injection or perfusion, brain microdialysis, autoradiography, and others are used at various stages of drug discovery and development to estimate CNS penetration and PK/PD correlation. Each technique has its own application with specific advantages and limitations.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2002
Page: [647 - 657]
Pages: 11
DOI: 10.2174/1389200023337063
Price: $58

Article Metrics

PDF: 20