Abstract: With the development of society, brain diseases have become an important factor affecting the quality of our life and health. It is difficult for general drug delivery systems to cross the blood-brain barrier to reach lesions, but the emergence of targeting drug delivery systems has achieved drug delivery in the brain to achieve therapeutic effects. Angiopep is a family of related peptides that can bind to the low-density lipoprotein receptor and mediate the permeability of the blood-brain barrier. Angiopep-2, one of the members of the peptide family, can be used for glial administration to improve drug delivery and accurately affect the lesion. Based on the biological properties and transport forms of angiopep-2, this article introduces its permeability to the blood-brain barrier and the therapeutic effects of targeting drug delivery.