Abstract: Central nervous system(CNS) diseases, which are caused by a variety of complex ischemic, hemorrhagic, inflammatory, neurodegenerative and developmental disorders, are quite common with poor therapeutic effects. One of the main obstacles to the treatment of CNS disease is the blood-brain barrier(BBB), which is a dynamic, adaptable and highly complex natural barrier to protect the brain. Many therapeutic agents have been discovered but cannot ultimately translate into effective clinical outcomes because they cannot cross the BBB. This paper reviews the drug delivery strategies across the BBB, including interfering with the BBB tight junctions or the exclusion system, improving BBB permeability of candidate molecules and carrier-coupled drug brain delivery, in the hope of providing reference for the development of CNS drugs.