Abstract: OBJECTIVE To investigate the targeted character of rifampicin polylactic acid/glycolic acid copolymer nanoparticles in lung after nebulized inhalation in rats. METHODS The rifampicin nanoparticles suspension (RFP-PLGA-NPs) and rifampicin suspension (RFP-Sol) were given to SD rats by nebulized inhalation, respectively. The concentrations of two formulations in lung at different time after nebulized inhalation were analyzed. Further more, their pharmacokinetic parameters were compared, and the targeted character was evaluated. RESULTS T_max of RFP-Sol and RFP-PLGA-NPs were (1.50±0.01) hand (2.00±0.08)h, C_max were (0.83±0.07)mg·L^-1 and (5.02±0.05)mg·L^-1, AUC₀→∞ were (6.24±0.24)mg·h·L^-1 and (35.80±6.34) mg·h·L^-1, CL were (4.81±0.18) L·h^-1·kg^-1 and (0.85±0.15)L·h^-1·kg^-1, respectively. Moreover, C_e and r_e of the two formulations in lung were analysed, which exceeded 1. CONCLUSION Compared with RFP-Sol, the nanoparticles after nebulized inhalation might elevate their distribution and slow their elimination in lung, and decrease the drug adverse reaction in rats, so as to improve the treatment efficacy of pulmonary tuberculosis.