Targeted drug delivery systems have been used to deliver drugs in the disease sites of the body. This may reduce potential side effects of drugs and improve their therapeutic effects. The blood brain barrier, formed by brain capillary endothelial cells, represents the major obstacle for drug entry into the central nervous system. Development of brain targeting drug delivery system help in the treatment of disorders related to brain. The most challenging research topic in pharmaceutical sciences is brain targeting drug delivery system. Most of the drugs do not reach brain effectively because of presence of Blood-Brain Barrier (BBB). There are various strategic approaches that have been proposed for brain drug delivery system. By localizing drugs at their desired site of action one can reduce toxicity and increase treatment efficiency. In response to the insufficiency in conventional delivery mechanisms, aggressive research efforts have recently focused on the development of new strategies to more effectively deliver drug molecules to the CNS. This review intends to detail the recent advances in the field of brain-targeting, rational drug design approach and drug delivery to CNS. To illustrate the complexity of the problems that have to be overcome for successful brain targeting, a brief intercellular characterization of the blood–brain barrier (BBB) is also included.
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