In Vitro Models to Study Blood-Brain Barrier Function

Abstract

The blood-brain barrier is formed by endothelial cells of brain capillaries. It protects the central nervous system from xenobiotics, dangerous metabolites, and toxins. This chapter gives a short overview about the history of blood-brain barrier research and the morphological and functional features of the barrier with special emphasis on the impact of ABC-transport proteins on drug permeability, as well as some examples to overcome or bypass export proteins, such as P-glycoprotein. Regulatory mechanisms underlying P-glycoprotein expression and function will be discussed. Ex vivo and in vitro models are introduced and methods to study drug permeation across the endothelial cell barrier will be described.