The treatment of brain diseases has been a major challenge since a long time. Although there are several potent drugs, which are highly therapeutic yet their efficiency is marred due to the presence of the Blood Brain Barrier (BBB). The BBB, which is present at the capillary level regulates and monitors the entry of all small and large molecules entering into the brain. Although this barrier is of immense importance to the brain in terms of safety, it becomes a hindrance when it comes to therapy because the drug molecules are unable to reach the brain. Various biomaterial-based strategies are being developed to overcome the BBB and deliver the drug into the brain. These include polymeric nanoparticles, liposomes, solid-lipid nanoparticles (SLNPs), nanogels, implants, etc. This review provides an overview on CNS disorders, BBB, and various delivery strategies available for biologists engaged in translational neuroscience, to target CNS.