Document Detail

Predicting blood-brain barrier permeability of drugs: evaluation of different in vitro assays.
MedLine Citation:
PMID:  12164375     Owner:  NLM     Status:  MEDLINE    
The ability of a drug to penetrate the blood-brain barrier (BBB) is essential for its use in the pharmaceutical treatment of CNS disorders. Five different in vitro methods to predict BBB permeability of drugs were compared and evaluated in the present study. All assays were performed with a consistent set of seven compounds and in the same physiological buffer to provide a basis for direct comparison of the results. Octanol-buffer and liposome-buffer partition coefficients were most conveniently obtained but failed to predict BBB permeability for certain drugs. The incorporation of drugs into lipid monolayers at the air-buffer interface was found to be a poor predictor of BBB permeability and was furthermore not considered suitable for screening due to the demanding experimental requirements. Permeability studies using Caco-2 cell monolayers provided a good correlation to an in vitro model of the BBB, which was based on primary cultured porcine brain capillary endothelial cells (PBCEC). However, differences in drug permeability between the intestine and brain derived cells were detected, limiting the advantages of the easy handling of the Caco-2 cell line compared to the more time-consuming primary culture of the BCEC.
C Lohmann; S Hüwel; H J Galla
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Publication Detail:
Type:  Evaluation Studies; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of drug targeting     Volume:  10     ISSN:  1061-186X     ISO Abbreviation:  J Drug Target     Publication Date:  2002 Jun 
Date Detail:
Created Date:  2002-08-07     Completed Date:  2002-12-23     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9312476     Medline TA:  J Drug Target     Country:  England    
Other Details:
Languages:  eng     Pagination:  263-76     Citation Subset:  IM    
Institut für Biochemie, Westfälische Wilhelms-Universität Münster, Germany.
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MeSH Terms
Blood-Brain Barrier / physiology*
Caco-2 Cells
Lipid Bilayers / metabolism
Membranes, Artificial*
Permeability / drug effects
Pharmaceutical Preparations / chemistry,  metabolism*
Reg. No./Substance:
0/Lipid Bilayers; 0/Liposomes; 0/Membranes, Artificial; 0/Pharmaceutical Preparations

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