Production of inclusion complexes containing corticosteroids by SAA process

Abstract

Slightly water-soluble drugs are frequently coprecipitated with a suitable carrier to speed up active principle ingredient (API) dissolution, improving its bioavailability. In this work, combined systems constituted by a corticosteroid and a cyclodextrin were micronized by Supercritical Assisted Atomization (SAA). When SAA processes corticosteroids alone, it is impossible to obtain micronized powders. The selected corticosteroids were prednisolone and dexamethasone, and a derivative of β-cyclodextrin was chosen as the carrier. The drug:cyclodextrin molar ratio and the initial solution concentration were varied to verify their influence on the powders’ particle size and particle size distribution. At all ratios and concentrations assessed, spherical micrometric particles were obtained. Under the optimized process conditions, compared to the unprocessed material, the dissolution time decreases from 18 h to 4 h in the case of prednisolone and from 22 h to 5 h in the case of dexamethasone.