Neurodegenerative diseases are a case of complex diseases that are disabled and fatal due to the great number of specific neurons lost, seriously endangering patients" safety and quality of life, and causing a heavy burden of public medical resources. In recent years, researchers have developed a large number of new drugs for neurodegenerative diseases, because small molecules derived from natural products have antioxidant, anti-inflammatory and neuroprotective functions, showing good preventive and therapeutic effects. However, due to the poor stability and low targeting of natural small molecule drugs, and more than 98% of them are not easy to penetrate the blood-brain barrier, it is difficult to effectively apply it to the clinic. Therefore, nano-formulations, which can improve the physical and chemical properties of small molecule drugs, increase the stability and tissue distribution, and improve the targeting of functional organs, are widely applied in the reconstruction of natural small molecule drugs. The aim of this paper is to summarize the research progress of nano preparation of natural small molecule drugs for neurodegenerative diseases, and to provide reference for the research and development of similar new drugs.