The blood-brain barrier provides the central nervous system with a unique protection against the toxic effects of many xenobiotics. This protection results from the unique anatomic and biological structure of the endothelium of blood vessels in the brain. The main features of the blood-brain barrier are the presence of tight intercellular junctions which strictly limit the diffusion of blood-borne solutes and cells into the brain and the polarized expression of transporters which specifically control the cerebral availability of nutrients, drugs or xenobiotics. Recent findings in molecular and cellular biology improved our knowledge of blood-brain barrier permeability and its regulation. The importance of these findings has been recently highlighted by the description of dysfunctions of the blood-brain barrier which could have an impact on the pathophysiology of several neurological diseases. This review focuses on recent advances in our understanding of blood-brain barrier biology and physiology, presenting the structural organization of the blood-brain barrier and the functional regulation of solute permeability and cellular transendothelial migration.