Interest of cylodextrins in spray-dried microparticles formulation for sustained pulmonary delivery of budesonide

The present study aim at developing cyclodextrin-based spray-dried microparticles containing a corticosteroid (budesonide) with an efficient lung delivery and efficacy. Complexation between budesonide and hydroxypropyl-beta-cyclodextrin (HPBCD) has been investigated and production of spray-dried powder was optimized based on a design of experiments. Wrinkled particles associated with a low bulk density and improved respirable fraction in comparison to a marketed product were obtained. An in vitro test showed that HPBCD is able to decrease the permeability of budesonide across the bronchial epithelium by a sustained release effect. In conclusion, this work reports that the use of cyclodextrin in the formulation of dry powder for inhalation is of a double interest as it both improves respirable fraction and lung residence time of budesonide.