Objective To explore the feasibility of brain-targeting intranasal administration with β-asarone microemulsion by nose-brain pathway. Methods The concentration of β-asarone in plasma and brain following nasal administration of β-asarone microemulsion(0.42 mL/kg) was measured by HPLC, taking the iv administration of self microemulsion injection as control. And the brain-targeting was evaluated by ratio of AUCbrain/AUCplasma. Results The ratio of AUCbrain/AUCplasma obtained after intranasal administration was significantly higher than that after iv administration. Conclusion The brain-targeting of β-asarone is better after intranasal administration which could become a new drug delivery system for the treatment of Alzheimer's disease.