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

Author: Feng M.Rose

Source: Current Drug Metabolism, Volume 3, Number 6, December 2002 , pp. 647-657(11)

Publisher: Bentham Science Publishers

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Abstract:

The amount of drug achieved and maintained in the brain after systemic administration is determined by the agent's 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 molecule's 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.

Keywords: blood-brain barrier; bbb; bbb penetration; cns penetration; pgp; mrp

Language: English

Document Type: Review article

DOI: 10.2174/1389200023337063

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