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In the study, a liposomal drug delivery system with targeting ligand (G-ligand) was developed for targeting the BBB.The feasibility of the BBB targeting liposome was evaluated by encapsulating an endogenous opioid peptide (EM-1), estimating its antinociceptive effect by hot-plate test, and quantifying EM-1 concentrations in the brain of mice.Results indicated that NG562 formulation could facilitate transporting EM-1 into the brain, thus enhance antinociceptive effects by blocking the μ-opioid receptor on neurons.