Prevalence and distribution of central nervous system (CNS) disorders in current global scenario are on an alarmingly higher phase, estimating around 24.3 million populations globally suffering from Dementia / Alzheimer's disease (AD) until 2015. A wide range of drugs have been discovered in last 3-4 decades for various neuronal disorders. However, the therapeutic success of these pharmaceuticals remains restricted as, the listed drugs for cerebral disorders, generally cannot cross the biological barriers of brain: Blood-brain barrier (BBB), and Blood-cerebrospinal fluid barrier (BCSFB), thus, limiting their reach to brain. Phyto pharmaceuticals are much favored over chemically fabricated drugs, due to their comparatively higher patient compliance and lesser adverse effects but they are equally prone to structural and chemical degradation hence, lowers their biological efficacy. These phenomena block the medication distribution towards the targeted origin site of disease and banning the passive diffusion of several compounds in CNS. Also, they're very sensitive to degradation and/or are metabolized to inactive derivatives in circulation. However, to attain the maximum therapeutic index of these potential drugs they need to be delivered through novel approaches where it can have a substantial impact on its effectiveness, absorption, distribution and efficacy. Also, in neurological disorders the direct targeting approach has gained immense consideration for drug delivery in brain due to its high efficacy and reduced side effects which is been effectively exhibited by intranasal drug delivery route by olfactory neural pathway. There are many natural products (extracts as well as, purified compounds) which have been worked upon by our research group for the neuronal disorders treatment and their efficacious delivery to the targeted site of brain, such as; crude extract of Curcuma longa (CLNPs), Centella asiatica (CANPs), Gingko biloba (GBME), Theobroma cacao (TCNGs) etc. and pure compounds like - Bilobalide, Quercetin, (-)-Epigallocatechin-3-gallate (EGCG), Catechin hydrate and Apocynin etc. We have developed the nanoformulations for these extracts and phytocompounds and assessed there therapeutic efficacy, stability and release kinetics in comparison to their conventional forms. Further, the in vitro cytotoxicity evaluation reports suggest that GBME has no significant cytotoxic effect on NB41A3 and RPMI2650 cell lines exposing them for 12 and 24 hrs to the experiment range of evaluation. Similarly, in vivo data indicates comparatively more neuroprotective efficiency of the optimised formulation (GBME) in comparison to the extract (EGB761) and positive standard (Reminyl) in Alzheimer’s induced mice model. In conclusion, the results and data expression of mentioned studies demonstrated that the developed formulations has an potential therapeutic effects on improving the pathological state of AD, and could be taken further as a promising candidate for clinical research to evaluate its efficacy in human Keywords: Nanomedicine, Novel drug delivery systems, Olfactory pathways, therapeutic index, Blood-brain barrier (BBB), Blood-cerebrospinal fluid barrier (BCSFB).