Diseases of the central nervous system are serious health concerns which have been poorly treated due to immense challenges involved in it. One of the major complexities involved is the inability of the drugs to reach their target site of action, primarily due to the presence of various CNS barriers like the blood brain barrier (BBB), blood-cerebrospinal fluid barrier, etc. Also, chronic use of many of the currently available therapeutic agents is known to produce multiple adverse effects resulting in several of these treatments being deemed as ineffective. Recently there has been an increased interest in understanding the role of nutraceuticals in various diseases due to a surge in demand for naturally derived bioactive remedies because of lower side effects associated with them. A few nutraceuticals have shown to possess neuroprotective action thus indicating their potential in treating various CNS diseases. However, limited bioavailability of these nutraceuticals along with limited permeability across the BBB are some of the major hindrances for its effective usage. Nanotechnology has proved to be an innovative solution to overcome this problem. Nano particle conjugated nutraceuticals have improved bioavailability leading to increased efficacy. In this chapter we investigate the different nutraceuticals with proven benefits for various CNS diseases and the role of nanonutraceuticals formulations in improving the efficacy of the same with specific focus on Alzheimer’s disease.