Recent progress in blood-brain barrier transportation research

Achieving high bioavailability and enhancing therapeutic effect in the brain are the major challenges for the development of central nervous systems (CNS)-active therapeutics because of complex physiology and restricted regulating function of the blood-brain barrier (BBB). With our advancement in understanding the physiological features of the BBB, various CNS-targeted drug delivery strategies have been developed, including BBB disruption, drug modification, and carrier (nanoparticles or cells)-based drug delivery systems to improve drug transport across the BBB to treat CNS disorders. This chapter provides overview about (1) the physiological properties and the transport mechanisms at the BBB and (2) our advancement in the development of different CNS-targeted drug delivery strategies. Further understanding transport systems of the BBB and pros and cons of current delivery approaches will provide valuable insight for developing effective and novel CNS-active therapeutics for brain disorders.