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By regulating their selective and specific absorption, efflux, and metabolism in the brain, the CNS controls brain homeostasis and the transit of endogenous and foreign substances. The mechanism which protects the brain from environmental chemicals, also prevent the entry of therapeutic chemicals to it. The delivery of molecules to the brain is hindered by several major barriers, such as the blood\u2013brain barrier (BBB), blood\u2010cerebrospinal fluid barrier (BCSFB), and blood\u2010tumor barrier. BBB is formed by the combination of cerebral endothelial cells, astrocytes, neurons, pericytes and microglia. It is a tight junction of capillary endothelial cells, preventing the diffusion of solute into the brain. BCSFB is the second barrier, located at the choroid plexus, separating the blood from cerebrospinal fluid (CSF). It is comparatively more permeable than BBB. An uneven distribution of microvasculature across the tumor interstitial compromises drug delivery to neoplastic cells of a solid tumor, resulting in spatially inconsistent drug administration. Nasal drug delivery to the brain is a method of drug delivery that tries to deliver therapeutic substances directly from the nasal cavity to the central nervous system including the brain. In this review, besides the role of barriers we have discussed in detail about approaches adapted to deliver drugs to the brain along with mechanisms through nasal route. Further, different commercial formulations, clinical trials and patents have been thoroughly elaborated to date. 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