Many pharmaceuticals cannot access brain, though, has potential for treatment and this is mainly due to the potential blood brain barrier. To have a successful delivery, the challenges of anatomical and physiological aspects of those barriers need to be addressed. Though a considerable efforts were made in convincing those barriers, still designing a suitable delivery remains a major challenge. This review lists various strategies for the drug delivery to the brain. Sophisticated approaches like intracerebral delivery, intranasal delivery, barrier disruptions, receptor mediated transport, prodrugs, chemical drug delivery and many more were discussed. Limitations of some strategies were also discussed. Understanding the strategies along with the suitability of the therapeutic agent to undergo those strategic modifications would certainly promises the success of a brain drug delivery program. This a review made here would help the researcher in understanding the barrier and further modifying the therapeutic agent for the suitable drug or delivery.