The blood–brain barrier (BBB) serves as a highly selective barrier between the blood and the central nervous system (CNS), and its main function is to protect the brain from foreign substances. This physiological property plays a crucial role in maintaining CNS homeostasis, but at the same time greatly limits the delivery of drug molecules to the CNS, thus posing a major challenge for the treatment of neurological diseases. Given that the high incidence and low cure rate of neurological diseases have become a global public health problem, the development of effective BBB penetration technologies is important for enhancing the efficiency of CNS drug delivery, reducing systemic toxicity, and improving the therapeutic outcomes of neurological diseases. This review describes the physiological and pathological properties of the BBB, as well as the current challenges of trans-BBB drug delivery, detailing the structural basis of the BBB and its role in CNS protection. Secondly, this paper reviews the drug delivery strategies for the BBB in recent years, including physical, biological and chemical approaches, as well as nanoparticle-based delivery technologies, and provides a comprehensive assessment of the effectiveness, advantages and limitations of these delivery strategies. It is hoped that the review in this paper will provide valuable references and inspiration for future researchers in therapeutic studies of neurological diseases.