Objective To study the pharmacodynamics and pharmacokinetics of inhaled dry powder of nanoparticles-in-microparticles system (NiMS) loaded with wheat germ agglutinin (WGA)-anchored salmeterol xinafoate (SalX) in mice. Methods The asthma model was established by subcutaneous and intraperitoneal injection of ovalbumin (OVA) in mice. WGA-SalX-NiMS powder was delivered to mice through airway dry powder inhalation. Reference method was applied in this study. The lung tissue and airway inflammation were examined, and the pharmacokinetics of SalX in the plasma and lung tissue of mice were studied after the administration of WGA-SalX-NiMS. The concentration-time data was analyzed using Sigma State statistical package. Results Compared with the model group, the counts of white cells, eosinophils, lymphocytes and macrophages in the bronchoalveolar lavage fluid (BALF) of mice in SalX-NiMS group and WGA-SalX-NiMS group showed a descending trend. The BALF counts of lymphocytes and macrophages in WGA-SalX-NiMS group were significantly less than those in SalX-NiMS group (P<0.05). The plasma pharmacokinetics parameters of mice were as follows: t_max 1.500 h, C_max 57.366 mg/L, t_1/2β 69.315 h, AUC_0-∞ 2 427.205 mg·L^-1·h, MRT_0-∞ 55.294 h for SalX-NiMS; t_max 1.000 h, C_max 62.581 mg/L, t_1/2β 69.315 h, AUC_0-∞ 4 071.838 mg·L^-1·h, MRT_0-∞ 75.094 h for WGA-SalX-NiMS. The pharmacokinetics parameters of lung tissue of mice were as follows: t_max 0.083 h, C_max 0.497 μg/mg, t_1/2β 11.231 h, AUC_0-∞ 3.936 μg·mg^-1·h, MRT_0-∞ 13.854 h for SalX-NiMS; t_max 0.083 h, C_max 0.796 μg/mg, t_1/2β 27.294 h, AUC_0-∞ 5.578 μg·mg^-1·h, MRT_0-∞ 26.330 h for WGA-SalX-NiMS. The drug concentrations of WGA-SalX-NiMS in both plasma and lung tissue were significantly higher than those of SalX-NiMS (P<0.05). Conclusion The drug release rate of SalX-NiMS is promoted and the drug concentrations in the plasma and lung tissue are increased after the modification with WGA, which contributes to the control and improvement of the airway inflammation during asthmatic attack.