Preparation of non-steroidal anti-inflammatory drug/β-cyclodextrin inclusion complexes by supercritical antisolvent process

Abstract

In this work, β-cyclodextrin (β-CD) was used as a carrier to produce inclusion complexes containing Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), namely nimesulide (NIM) and ketoprofen (KET), by Supercritical AntiSolvent (SAS) process. The effect of different parameters, such as pressure, overall concentration of solutes in the liquid solution, and NSAID/β-CD molar ratio, on the morphology and size of the composite particles, was investigated. Well-defined microparticles at different NSAID/β-CD molar ratios were produced, managing to increase this ratio up to 2/1 mol/mol. The formation of NIM/β-CD and KET/β-CD inclusion complexes was demonstrated through different analytic techniques, such as Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The attainment of inclusion complexes induced the enhancement of the NSAID dissolution rate up to about 21 and 7 times in the case of SAS NSAID/β-CD 2/1 mol/mol if compared to unprocessed NIM and KET, respectively. SAS process was proved to be effective in the preparation of inclusion complexes by using β-CD for an accelerated drug release.