Drug delivery to the brain, restricted by the blood-brain barrier (BBB), remains one of the major obstacles in central nervous system (CNS) drug development. Solute carriers and ATP-binding cassette family (ABC) transporters expressed at the BBB play crucial roles in drug delivery to the brain. Knowledge about brain transporters and the receptors expressed has opened up new opportunities for improving drug delivery to the brain and understanding the pathogenesis of CNS diseases. This Special Issue, entitled the "Roles of Transporters and Receptors in Drug Delivery to the Brain in Health and Disease", aims to provide information about the latest developments in the field of transporter-mediated drug delivery to the brain, the roles of transporters and receptors in CNS diseases, as well as advances in the methodologies for the evaluation of carrier-mediated drug delivery to the brain.