Neurological disorders represent one of the major health concerns worldwide. Yet currently employed
treatment strategies have not been very successful in the treatment of many of these disorders. One of the root
causes of this lack of success is that many pharmaceutically active compounds are unable to reach their target sites
of action inside the body. The delivery of substances from systemic circulation to the desired site of action, namely
central nervous system (CNS), is hindered by CNS extracellular and intracellular barriers. One promising approach
to circumvent these barriers is the use of nanoscaled drug delivery systems. These nanosized drug carriers display
various advantages over other conventional drug delivery methods such as high drug loading capacity, targeted action,
reduced toxicity, and increased therapeutic effect. Nano-neuroscience is thereby emerging as an exciting field
of study and a promising future direction for the delivery of therapeutics to their targeted site of action inside the CNS for the treatment
of various neurological and psychiatric disorders. Here, we will first discuss the general pharmacokinetics of therapeutics depending on
the route of administration, drawbacks of conventional drug delivery systems and challenges for CNS drug delivery, namely CNS barriers.
Next, a short overview of the strategies to circumvent these barriers will be given. Finally, nanotechnology and its emerging use as
drug delivery systems will be discussed. This includes the advantages of nanoparticles over other conventional drug delivery systems;
production of nanoparticles and their designing as an effective drug carrier; various types of nanoparticles; and some examples of their
efficient use in the delivery of bioactive substances, and in the treatment of neurological disorders mainly Alzheimer’s disease, brain tumors
and neuroAIDS. Lastly, a future perspective on the use of nanotechnology in CNS drug delivery will be highlighted.