Effects of lipids on dissolution of poorly water-soluble drugs

Abstract

Despite the significance of fat-rich food/drug interactions, there is an incomplete understanding of the influence of ingested lipids on orally delivered hydrophobic drug bioavailability. In order to determine the impact of lipid and lipid digestion on drug dissolution and absorption, an updated in vitro lipid digestion model has been designed based on knowledge of gastrointestinal contents. The digestion kinetics sensitivity to key parameters, including pH, calcium concentration, and lipid substrate, has been studied. In vitro lipolysis experiments have been coupled with several techniques, such as dynamic light scattering (DLS), and electron paramagnetic resonance (EPR), to characterize respectively: size and morphology of colloidal particles, and dynamic drug partitioning between phases.