The aim of this study was to develop a blood-brain barrier (BBB) permeability model, which is applicable to the drug discovery phase. A new refined ex vivo insect-based BBB screening model that uses intact, viable whole brain under “in vitro”-like exposure conditions is described in this article. The model uses intact brains from desert locusts, which are placed in a well containing the compound solubilized in an insect buffer. After a limited period of time, the brain is removed, and the compound concentration in the brain is measured by liquid chromatography-mass spectrometry. Twenty-five known drugs were studied, and the results found that the insect brain uptake correlated with in situ perfusion data obtained in vertebrates. Moreover, this study shows that the insect model is able to identify P-glycoprotein substrates.
See article at J Pharmacol Exp Ther 2013 346:211–218.
- Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics