Central nervous system (CNS) disorders have been incorporated into our daily lifestyle now and in general, are faced by people of all age-groups and affect both men and women across the world. The drugs for the treatment of these disorders must overcome the blood-brain barrier, serious obstacle for the permeation of drugs that require CNS action. Rapid development of various nanosystems employed for nano-based drug delivery systems have great potential to facilitate the movement of drugs across all barriers and thus these drug carriers have been extensively studied as a strategy of direct drug delivery to the CNS. This contribution is focused on the effects and CNS targeting of nanoscale formulations containing drugs such as antiepileptics, antipsychotics, anxiolytics, antidepressants as well as drugs applied for the treatment of schizophrenia and Parkinson’s and Alzheimer’s diseases. The benefits connected with their application (e.g., reduction of required drug dose at bioavailability increase, reduced side effects due to decreased toxicity against nontarget cells, prolongation of time in circulation) are highlighted as well.