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

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: http://dx.doi.org/10.2174/1389200023337063

Publication date: 2002-12-01

• Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:
  
  In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.

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• In this Subject: Anatomy & Physiology ,  Pharmacology
• By this author: Feng M.Rose

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