Betulin, a triterpenoid present in birch bark, possesses a broad spectrum of biological activity. Its bioavailability is limited by low solubility in water whereas the shape and size of particles are not suited for administration via inhalation. One of the main drawbacks of inhalation preparations is low bioavailability because of the sedimentation of particles in the mouth. The present work was aimed at a biopharmaceutical study of nanosystems with betulin for administration via inhalation. Nanosystems were characterized by photon-correlation spectroscopy, differential scanning calorimetry, and x-ray powder diffraction. In addition, their dissolution profile was obtained by the Dissolution test. It is established that the obtained nanosystems with betulin exhibit high bioavailability, have optimal physicochemical properties for inhalation administration, and ensure deposition of betulin in the lower part of the respiratory tract.