Alzheimer's disease (AD) is the multifarious progressive neuro-degeneration
related dementia state among the elders. In fact, number of drugs with different
mechanistic prospective were clinically developed and currently under R & D for the
symptomatic treatment as well as disease-modifying management of AD. Unluckily,
effective and safe delivery of drug in Alzheimer's is restricted due to the presence of
biological as well as physiological barriers like blood–brain barrier (BBB), blood–
cerebrospinal fluid barrier (BCSFB) and p-glycoproteins. Advancement in nanotechnology
based drug delivery systems over the last decade exemplifies effective brain targeting
by delivering the drugs at a constant rate that can be extended even up to months. Till
recently, various nanomedicines such as polymeric and metallic nanoparticles, SLN,
liposomes, micelles dendrimers, nanoemulsions and carbon nano-tube etc have been
investigated for effective brain targeting of the drugs particularly in the treatment and
diagnosis of AD. Here in this review, we given an account of different barrier in brain
drug delivery and possible nanotechnology based strategies that can deliver drugs across
the CNS barriers in AD. In addition, we illustrate the typical and new cholinesterase
inhibitors for the management of AD, its clinical relevance and the challenges
associated with their bioavailable brain delivery. Success of nanomedicines in effective
therapeutic targeting in CNS with reference to literatures including the nanomedicines
as the novel carrier of cholinesterase inhibitors anti-AD has also covered.