Due to the presence of the blood-brain barrier, there is limited drug access into the brain. In order to overcome
this challenge, various strategies have been developed to enhance penetration of drugs into the brain. Of these, the most
frequently used are pharmacological technologies or comparable methods being developed for brain-targeting drug
delivery using receptor- or adsorptive- or transporter-mediated transcytosis and the nose-to-brain route. It goes without
saying that exploration of Brain-targeting drug delivery systems has created another potential option for the treatment of
central nervous system diseases. In addition to above methods, other technologies for brain-targeting drug delivery (e.g.
chemical delivery systems, prodrugs, pharmacological disruption of the BBB and inhibition of drug efflux by P-glycoprotein)
are also summaried in this review.
Keywords: Blood-brain barrier, brain-targeting drug delivery systems, receptor-mediated transcytosis, adsorptive-mediated
transcytosis, transporter-mediated transcytosis, nose-to-brain, chemical delivery systems, prodrugs, P-glycoprotein, Targeting drug delivery, colloidal drug, harmful blood-borne substances, small molecule drugs, endothelium cells
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