Abstract
We prepared rifampicin (RFP)/poly (lactic-co-glycolic acid) (PLGA) nanoparticle-containing mannitol (MAN) microspheres for inhalation therapy of tuberculosis using a four-fluid nozzle spray drier in one step. The uptake of RFP by alveolar macrophages in the lungs of rats from the RFP/PLGA microspheres was very small. The uptake of RFP from the RFP/PLGA nanoparticles, however, was larger because the nano-sized PLGA particles could be retained in the deeper part of the lungs. This study shows that it is feasible to prepare RFP/PLGA nanoparticle-containing microspheres using a four-fluid nozzle spray drier in one step, and that the particles are retained in the lungs for prolonged periods and targeted to alveolar macrophages.