The blood-brain barrier in humans significantly restricts the effective delivery of drugs into the brain, resulting in poor therapeutic efficacy and difficulty in brain disease management. In recent years, innovative strategies and novel preparations have been studied and developed in order to circumvent the blood-brain barrier, achieve efficient drug entry into the brain, minimize the incidence of peripheral adverse effects, and bring significant therapeutic outcomes to patients. This review summarizes some key development strategies for treating encephalopathy, to provide some insights for the development of the next generation of drugs.