Spinal cord injury (SCI) is a neurological disorder that can lead to loss of perceptive and athletic function due to the severe nerve damage. To date, pieces of evidence detailing the precise pathological mechanisms in SCI are still unclear. Therefore, drug therapy cannot effectively alleviate the SCI symptoms and faces the limitations of systemic administration with large side effects. Thus, the development of SCI treatment strategies is urgent and valuable. Due to the application of nanotechnology in pharmaceutical research, nanopharmaceutical-based regenerative medicine will bring colossal development space for clinical medicine. These nanopharmaceuticals (i.e. nanocrystalline drugs and nanocarrier drugs) are designed using different types of materials or bioactive molecules, so as to improve the therapeutic effects, reduce side effects, and subtly deliver drugs, etc. Currently, an increasing number of nanopharmaceutical products have been approved by drug regulatory agencies, which has also prompted more researchers to focus on the potential treatment strategies of SCI. Therefore, the purpose of this review is to summarize and elaborate the research progress as well as the challenges and future of nanopharmaceuticals in the treatment of SCI, aiming to promote further research of nanopharmaceuticals in SCI.