Drug delivery to the brain is an engaged research topic in the field of nanomedicine. The passage of therapeutics into the brain parenchyma is more complicated than other body tissues due to it is limited by restrict barrier structure called blood-brain barrier (BBB). Nanotechnology holds great promise to overcome the BBB and thereby enable treatment of neurodegenerative diseases. Nanocarriers have been investigated several times as effective brain drug delivery systems in the past few decades. Physicochemical properties and surface modifications of these carriers play a significant role in terms of brain up-taking of nanocarriers. Chemical structures of possible nano sized drug delivery systems have an importance in terms of interactions between cell membranes of brain endothelial cell lines and these interactions can be modified with surface coating strategies using suitable agents. Particle size, surface charge and total molecular mass are also crucial issues which require special attention in order to better understand appropriate properties of nanocarriers to overcome the BBB structure. Different strategies have been demonstrated to facilitate the passage of nanoparticles into the brain parenchyma including attachment of targeting ligands on the nanoparticles’ surfaces; this attempt provides site specific action in the brain tissues. This study aims to provide a review of nanocarriers for effective brain drug delivery, in the light of current literature.