The major problem in drug delivery to the brain is the presence of the blood-brain barrier (BBB) which limits drug penetration even if in certain pathological situations the BBB is partly disrupted. Therefore, various strategies have been proposed to improve the delivery of drugs to this tissue. This review presents the status of the BBB in healthy patients and in pathologies like neurodegenerative, cerebrovascular and inflammatory diseases. The second part of this article aims to review the invasive and non-invasive strategies developed to circumvent the BBB and deliver drugs into the brain. The use of nanotechnologies (liposomes, nanoparticles) is especially discussed in the ultimate part of the review evidencing their potentiality as non-invasive technique in the brain delivery of drugs with the possibility to target specific brain tissue thanks to ligand linked to carrier surface.