In recent years, the researchers and drug designers have given growing attention to new nanotechnology strategies to improve drug delivery to the central nervous system (CNS). Nanotechnology has a great potential to affect the treatment of neurological disorders, mainly Alzheimer’s disease, Parkinson’s disease, brain tumors, and stroke. With regard to neurodegeneration, several studies showed that nanomaterials have been successfully used for the treatments of CNS disorders. In this regard, nanocarriers have facilitated the targeted delivery of chemotherapeutics resulting in the efficient inhibition of disease progression in malignant brain tumors. Therefore, the most efficacious application of nanomaterials is the use of these substances in the treatment of CNS disease that enhances the overall effect of drug and highlights the importance of nano-therapeutics. This study was conducted to review the evidence on the applications of nanotechnology in designing drug delivery systems with the ability to cross through the blood-brain barrier (BBB) in order to transfer the therapeutic agents to the CNS.