Many brain diseases pose serious challenges to human life. Alzheimer's Disease (AD) and Parkinson's Disease (PD) are common neurodegenerative diseases that seriously threaten human health. Glioma is a
common malignant tumor. However, drugs cannot cross physiological and pathological barriers and most therapeutic drugs cannot enter the brain because of the presence of the Blood-brain Barrier (BBB) and Blood-
-brain Tumor Barrier (BBTB). How to enable drugs to penetrate the BBB to enter the brain, reduce systemic
toxicity, and penetrate BBTB to exert therapeutic effects has become a challenge. Nanosuspension can successfully formulate drugs that are difficult to dissolve in water and oil by using surfactants as stabilizers, which is
suitable for the brain target delivery of class II and IV drugs in the Biopharmaceutical Classification System
(BCS). In nanosuspension drug delivery systems, the physical properties of nanostructures have a great impact
on the accumulation of drugs at the target site, such as the brain. Optimizing the physical parameters of the
nanosuspension can improve the efficiency of brain drug delivery and disease treatment. Therefore, the key
challenges, influencing factors, and future perspectives of nanosuspension in enhancing brain drug delivery
are summarized and reviewed here. This article aims to provide a better understanding of nanosuspension formulation technology used for brain delivery and strategies used to overcome various physiological barriers.