DRUG TRANSPORT TO THE BRAIN - COMPARISON BETWEEN IN-VITRO AND IN-VIVOMODELS OF THE BLOOD-BRAIN-BARRIER

The aim of the present studies was to compare the transport of drugs u sing two in vitro models routinely used in our laboratories: a primary culture of brain microvessel endothelial cells and a coculture of bra in capillary endothelial cells and astrocytes. For this purpose we sel ected a set of compounds corresponding to a wide range of lipid solubi lity. Additionally the in vitro results were compared to in vivo resul ts obtained with the single carotid injection, and a good correlation between in vivo extraction ratios (E(t)) and in vitro permeability coe fficients (P-e) was shown as indicated by the Spearman's correlation c oefficient (r = 0.90 and r = 0.96 for primary culture and coculture, r espectively). The studies show that the use of brain capillary endothe lial cells together with astrocytes is slightly more predictive and si gnificantly easier than the use of primary cultured brain microvessels .