Treating central nervous system (CNS) disease is a huge challenge because of the presence of various obstacles. These obstacles, including blood-brain barrier as the major one, prevent the drug from penetrating into brain, which results in the low efficacy of many potential therapeutic agents. Therefore, a variety of novel strategies have been proposed to overcome the barriers and deliver drugs in a sufficient quantity to the CNS. One of the possibilities is drug delivery to the brain using nanoparticles. Nanoparticles delivery systems can penetrate the barriers and target to the CNS by modifying the surface and attaching groups to them, besides, the methods of preparation are generally simple and easy to scale-up. This review intents to detail the nanoparticles used for drug delivery to the CNS.