The current epoch has witnessed a lifestyle impregnated with stress, which is a major cause of several
neurological disorders. High morbidity and mortality rate due to neurological diseases and disorders have generated
a huge social impact. Despite voluminous research, patients suffering from fatal and/or debilitating CNS diseases
such as brain tumors, HIV, encephalopathy, Alzheimer’s, epilepsy, Parkinson’s, migraine and multiple sclerosis
outnumbered those suffering from systemic cancer or heart diseases. The brain being a highly sensitive neuronal
organ, has evolved with vasculature barriers, which regulates the efflux and influx of substances to CNS.
Treatment of CNS diseases/disorders is challenging because of physiologic, metabolic and biochemical obstacles
created by these barriers which comprise mainly of BBB and BCFB. The inability of achieving therapeutically active
concentration has become the bottleneck level difficulty, hampering the therapeutic efficiency of several promising drug candidates
for CNS related disorders. Parallel maturation of an effective CNS drug delivery strategy with CNS drug discovery is the need of the
hour. Recently, the focus of the pharmaceutical community has aggravated in the direction of developing novel and more efficient drug
delivery systems, giving the potential of more effective and safer CNS therapies. The present review outlines several hurdles in drug delivery
to the CNS along with ideal physicochemical properties desired in drug substance/formulation for CNS delivery. The review also
focuses on different conventional and novel strategies for drug delivery to the CNS. The article also assesses and emphasizes on possible
benefits of biomaterial based formulations for drug delivery to the CNS.