Abstract

The blood-brain barrier is a vital protective barrier that shields the central nervous system from potentially harmful substances circulating in the bloodstream. At the heart of its functionality lie drug transporters-specialized proteins embedded in BBB endothelial cells that regulate the passage of molecules between the bloodstream and the brain. This article explores the intricate role of drug transporters within the BBB, presenting their dual nature as both protective agents and challenges in drug delivery. Efflux and influx transporters shape the brain’s exposure to therapeutic agents, posing both opportunities and obstacles. Efflux transporters safeguard the brain by actively pumping out xenobiotics, yet their presence limits drug efficacy by reducing brain penetration. Influx transporters, facilitating nutrient and neurotransmitter transport, offer potential for enhanced drug delivery. This review discusses strategies to overcome transporter-mediated barriers, including transporter inhibitors, prodrug designs, and innovative nanotechnological approaches. Achieving a delicate balance between harnessing the protective properties of drug transporters and circumventing their restrictive impact is essential for advancing targeted therapies for neurological disorders.