Evaluation of the MDR-MDCK cell line as a permeability screen for the blood-brain barrier.

The objectives of this study were to (1) characterize MDR-MDCK monolayers as an in vitro model to predict brain uptake potential; (2) examine the ability of MDR-MDCK monolayers to identify the brain uptake potential of compounds that interact with P-glycoprotein (P-gp). The study measured the bi-directional transport of 28 compounds across MDR-MDCK monolayers. The brain uptake of a subset of the compounds was determined in the rat brain perfusion model.