Tailoring of P-glycoprotein for effective transportation of actives across blood-brain-barrier.

P-Glycoprotein serves as a gatekeeper in the blood-brain-barrier wherein, it shows a vital part in the elimination of xenobiotics, drugs, foreign molecules etc. and guards the central nervous system from infections and external toxic molecules by functioning as an efflux transporter. It plays an essential role in various brain-related conditions like Parkinsonism, Alzheimer's disease, depression, cancer, etc. and terminates the entry of therapeutic agents across blood-brain-barrier which remains a significant challenge serving as major hindrance in pharmacotherapy of disease. The physiological structure and topology of P-glycoprotein and its relation with blood-brain-barrier and central nervous system gives an idea for targeting nanocarriers across the barrier into brain. This review article provides an overview of current understanding of the nanoformulations-based P-gp trafficking strategies like nanocarriers, stem cell therapy, drugs, substrates, polymeric materials, chemical compounds as well as naturally occurring active constituents for improving drug transport in brain across blood-brain-barrier and contributing in effective nanotherapeutic development for treatment of CNS disorders.