The blood-brain barrier (BBB) is a complex biological system that consists of endothelial cells, pericytes and astrocytes, which are involved in the induction and maintenance of its physiological and ultrastructural characteristics. The BBB plays a primordial role in isolating the cerebral parenchyma as well as in controlling brain homeostasis by its selective permeability to nutriments and other molecules flowing through the cerebral microcapillaries. A better knowledge of this system is crucial in order to improve the efficiency of brain penetration by drugs, and in order to prevent BBB opening, leading to brain edema, in physiopathological situations such as brain ischemia, trauma or inflammatory processes.