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The challenges of drug delivery to the brain can be overcome by chemical and pharmaceutical approaches; current research is focused on developing novel drug delivery systems for both local and systemic actions. Nose-to-brain targeting has vast potential for commercialization, as these systems allow the lowering of doses, by direct targeting of the active molecule that provides easy attainment of the effective concentration at the target site. Consequently, these systems are being explored for the delivery of biologically active molecules, to treat the ailments of the CNS and various proteins, amino acids and hormones.

The treatment of various central nervous system (CNS) diseases has been challenging, despite the rapid development of several novel treatment approaches. The blood–brain barrier (BBB) is one of the major issues in the treatment of CNS diseases, having major role in the protection of the brain but simultaneously constituting the main limiting hurdle for drugs targeting the brain. Nasal drug delivery has gained significant interest for brain targeting over the past decades, wherein the drug is directly delivered to the brain by the trigeminal and olfactory pathway. Various novel and promising formulation approaches have been explored for drug targeting to the brain by nasal administration. Nanoemulsions have the potential to avoid problems, including low solubility, poor bioavailability, slow onset of action, and enzymatic degradation. The present review highlights research scenarios of nanoemulsions for nose-to-brain delivery for the management of CNS ailments classified on the basis of brain disorders and further identifies the areas that remain unexplored. The significance of the total dose delivered to the target region, biodistribution studies, and long-term toxicity studies have been identified as the key areas of future research.

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