Case study: adapting in vitro blood–brain barrier models for use in early-stage drug discovery

Several parameters influencing the brain distribution of compounds must be considered when designing potential neuropharmaceuticals in early-stage drug discovery. The blood–brain barrier (BBB) represents an obstacle for drug penetration into the brain. Many in vitro BBB models have proven useful for...

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Bibliographic Details
Published in:Drug discovery today 2012-04, Vol.17 (7-8), p.285-290
Main Authors: Vandenhaute, Elodie, Sevin, Emmanuel, Hallier-Vanuxeem, Dorothée, Dehouck, Marie-Pierre, Cecchelli, Roméo
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Biological Transport
Blood-Brain Barrier - metabolism
Case-Control Studies
Drug Discovery
General pharmacology
Humans
Medical sciences
Models, Biological
Pharmaceutical Preparations - chemistry
Pharmaceutical Preparations - metabolism
Pharmaceutical technology. Pharmaceutical industry
Pharmacokinetics
Pharmacology. Drug treatments
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Summary:Several parameters influencing the brain distribution of compounds must be considered when designing potential neuropharmaceuticals in early-stage drug discovery. The blood–brain barrier (BBB) represents an obstacle for drug penetration into the brain. Many in vitro BBB models have proven useful for predicting the BBB permeation rate, but do not meet all criteria for use in early-stage drug discovery: feasibility, rapidity, reliability and a low requirement for human resources. To meet this demand, we have developed a robust, higher-throughput, cell-based model exhibiting BBB features (low paracellular permeability, functional efflux pumps and the correct endothelial phenotype). This system comes in a ready-to-use, frozen format, appropriate for in-house use by large pharmaceutical firms and small biotech companies during early-stage drug discovery.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2011.10.006