Production of pharmaceutical and nutraceutical formulations for bioavailability improvement using Supercritical Assisted Atomization

Abstract

Industrial interest is focused on the development of new pharmaceutical and nutraceutical formulations aimed at the enhancement of bioavailability of poorly water-soluble active compounds. Various factors influence the bioavailability of an active principle in a solid formulation, such as the particle size distribution, the solid state and the morphology. In order to enhance bioavailability, two different approaches were investigated in this thesis: particle size reduction of pure ingredients and production of amorphous formulations consisting of the dispersion of the hydrophobic molecule into a hydrophilic matrix (carrier). Supercritical fluid (SCFs) based techniques demonstrated to be a valid alternative to traditional processes, given the SCFs specific properties, such as liquid-like density, very fast mass transfer similar to gas, near-zero surface tension, effective solvent elimination. Among SCFs techniques, Supercritical Assisted Atomization (SAA) was successfully used to produce controlled micro and sub-microparticles of pure compounds, but also composite systems. The enhancement of bioavailability of active ingredients is still poorly investigated in the SAA literature. The ability of the SAA process in crystallinity control and particle size reduction is investigated in order to enhance the bioavailability of new active principles, often not feasible through conventional methods. This Ph.D. work is the most recent advance in the application of this supercritical fluid technology for the production of new and stable pharmaceutical and nutraceutical formulations. ... [edited by Author]