Spray drying of amorphous ibuprofen nanoparticles for the production of granules with enhanced drug release

Abstract

This work investigates formulation strategies for the production of pharmaceutical powders out of precipitated API (active pharmaceutical ingredient) nanoparticles. In order to accomplish this challenge, composite granules were designed via two distinct formulation strategies with the final goal of producing pharmaceutical powders with enhanced bioavailability. On the one hand, lactose granules were prepared by embedding secluded ibuprofen nanoparticles (particle size of ibuprofen: 100nm) in a lactose matrix via spray drying. On the other hand, silica granules were obtained by encasing ibuprofen nanoparticles in a nanoparticulate silica shell (primary particle size of silica: 40nm). Afterwards, granules were analysed by means of dissolution tests with a view to comparing different loading procedures regarding drug release. Furthermore, differential scanning calorimetry (DSC) measurements were used to prove the solid state, amorphous or crystalline, of APIs. Additionally, scanning electron microscopy (SEM) images enabled to characterize the morphology of the granules.