A procedure has been developed to prepare the nanosomal formulations of rifampicin and gatifloxacin based on a copolymer of lactic and glycolic acids. Murine experiments tested the antituberculosis activity of the drugs versus conventional drugs. It evaluated their bacteriostatic activity against Mycobacterium tuberculosis in the blood and lung homogenates taken at definite time points after the experimental nanosomal samples of rifampicin or gatifloxacin and their standard dosage forms were administered to mice. The antituberculosis activity of nanosomal rifampicin in the lung was ascertained to be twice higher than that of reference rifampicin within 2 hours after intravenous injection. As compared to the enteral administration of gatifloxacin substance in particular, the intravenous injection of nanosomal gatifloxacin was shown to provide a higher bacteriostatic activity against M. tuberculosis in the blood and lung tissue.