Prediction of in situ Blood-Brain Barrier Permeability using BBB PAMPA Model

Central nervous system (CNS)-targeting drugs need to cross the blood-brain barrier (BBB) in order to reach their therapeutic receptors inside the brain. If a reliable, reasonably low-cost, compound-sparing, and high-throughput method could be developed to predict the potential of pharmaceutical discovery compounds penetrating the BBB, then such a product would be an important contribution to the assortment of the discovery tools available for pharmaceutical industry. This study presents new developments achieved in BBB lipid formulation for the PAMPA assay and comparison between BBB PAMPA and recently published rat in situ perfusion permeability data. It also discusses applicability of commercially available pre-coated PAMPA plates from BD Biosciences for the prediction of in situ rodent brain perfusion uptake kinetics.

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