AIDS is caused by the infection of the human immunodeficiency virus (HIV). Against the mechanisms of HIV-1 invasion and transmission, as well as other possible mechanisms that inhibit HIV-1, we have obtained a series of membrane fusion inhibitors such as C22 and M3 peptides against HIV-1. However, peptide and protein drugs generally face difficulties and shortcomings in gastrointestinal administration, such as acid hydrolysis in the stomach, poor permeability of gastrointestinal mucosa, and low lipid solubility affecting absorption. Chitosan oligosaccharides are oligomers of glucosamine with 2 to 20 amino glucose units connected together, prepared through degradation using biotechnological methods from chitosan. They play an important role in enhancing immunity, reducing blood lipids and blood sugar, preventing and controlling the metastasis of cancer cells, and inhibiting cell aging. This invention aims to provide the application of chitosan oligosaccharides and their derivatives as carriers for anti-HIV-1 peptide drugs. As a carrier for peptide drugs, It can increase the bioavailability of peptide drugs with low absorption rates; control the release of peptide drugs; reduce irritation to the gastrointestinal mucosa; maintain stability of peptide drugs in vivo; and improve the targeting of the drug.