Background: Neuropsychiatric diseases primarily characterized by dementia stand third in the global list
of diseases causing disability. The poor water solubility, erratic oral absorption, low bioavailability, poor intestinal
absorption, and the impeding action of the blood-brain barrier (BBB) are the major factors limiting the therapeutic
feasibility of the antipsychotics. Only a small percentage of antipsychotics reaches the therapeutic target site, which
warrants administration of high doses, consequently leading to unwanted side-effects. Hence the main struggle for
the effective treatment of neuropsychiatric diseases occurs “at the gates” of the brain, which can be mitigated with
the use of a nanotechnology-based platform.
Methods: The goal of this review is to undertake a comprehensive study about the role of lipid nanoformulations in
facilitating the delivery of antipsychotics across BBB along with the available in vitro and in vivo evidence.
Results: Lipid nanoformulations have attained great popularity for the delivery of therapeutics into the brain. Their
nanosize helps in overcoming the biological barriers, thereby providing easy BBB translocation of the drugs. Besides,
they offer numerous advantages like controlled and targeted drug release, minimizing drug efflux, long storage
stability, augmented bioavailability, and reduced adverse drug effects to attain an optimal therapeutic drug concentration
in the brain. Moreover, employing alternative routes of administration has also shown promising results.
Conclusion: Thus, it can be concluded that the lipid nanoformulations bear immense potential in overcoming the
challenges associated with the treatment of neuropsychiatric disorders. However, the area warrants further clinical
studies to ensure their commercialization, which could revolutionize the treatment of neuropsychiatric diseases in the