Nanosomal formulation of moxifloxacin has been prepared by anionic polymerization of poly(butyl-2-cyanoacrylate) in the presence of the drug. Poly(butyl-2-cyanoacrylate) nanoparticles enables effective sorption of moxifloxacin with a high total content and considerable capacity of nanoparticles (>45%). The influence of the reaction parameters such as pH and drug-to-polymer ratio on the characteristics of the nanoparticles has been studied. Efficacy of the novel formulation has been evaluated in mice infected withM. tuberculosis. It is shown that the efficacy of the proposed nanosomal formulation for intravenous administration evaluated by a decrease in the mycobacteria count in lungs is more than twice greater as compared to that of a reference preparation.