The blood-brain barrier (BBB) effectively blocks most drugs from entering the central nervous system, posing significant challenges to the treatment of brain diseases, such as cerebrovascular disorders, neurodegenerative conditions, and brain tumors. In recent years, biomimetic braintargeted drug delivery systems (BBDDSs) have garnered substantial attention for their potential to overcome these obstacles. BBDDSs employ natural biological materials in combination with synthetic nanoparticles to create delivery systems that mimic endogenous biological processes, enabling the penetration of the BBB and facilitating brain-targeting efficacy. This paper reviews the preparation of BBDDS using cell membranes, proteins, lipoproteins, peptides, nanovesicles, and viruses, introduces their applications in various diseases, and outlines current challenges and future prospects for the use of BBDDS in therapeutic interventions.