Abstract: Intracerebral delivery of drugs for central nervous system disease therapy is usually limited by the blood-brain barrier. As a non-invasive way of brain-targeted drug delivery, transnasal administration can bypass the blood-brain barrier to achieve direct and efficient drug delivery to the brain, which shares great applicable potential in the treatment of central nervous system disease. However, barriers like nasal cilia clearance limit intranasal drug delivery. Derived from the development of nanoscale drug delivery technology, the intranasal nanoscale drug delivery system has brought new hope for the treatment of central nervous system disease. To provide an insight into developing intranasal nanoscale drug delivery system for central nervous system disease therapy, this review summarizes the nose-to-brain pathways, characteristics and application progress of common intranasal nanoscale drug delivery systems.