Delivery of the bioactives to the brain is the utmost challenging task to cope with brain diseases. Brain is protected with blood brain barrier, blood-CSF barrier and efflux systems, which controls the entry of body as well as foreign compounds to access the brain cells. Only nutrients, which are essential for normal metabolism, can enter into the brain. In the shadow of this fact new strategies are being investigated to facilitate the entry of administered therapeutic compound into the brain. Active targeting is a evolving approach, which uses ligand and suitable carrier for the site-specific delivery and is being recently achieved by the use of nanocarriers. These nanocarriers are nanosized systems, which act as a cargo for the encapsulated drugs. At the same time, endo- or exogenous ligand can be attached to these nanocarriers to recognize specific receptors on brain capillary endothelium leading to delivery of drug in the vicinity of brain cells. Their potential is under immense investigation to increase the therapeutics outcome in the treatment of brain related problems. This review deals with the recent advances in nanocarriers based novel strategies for effective brain specific delivery.