Solid dispersions of quercetin-PEG matrices: Miscibility prediction, preparation and characterization

Abstract

Quercetin is a bioflavonoid compound with low water solubility in both foods and the gastrointestinal tract, which limits the exploitation of its health-promoting properties. This study aims to formulate solid dispersions (SDs) of quercetin with hydrophilic polyethylene glycol PEG matrices, using the melt-mixing method, to improve the dissolution and antioxidant activity of quercetin. Initially, the total Gibbs free energy for different binary mixtures was modelled to predict the miscibility of the compounds. Then, the physicochemical properties of the formulated SDs were characterised and dissolution tests and antioxidant activity measurements were performed in vitro to evaluate the improved profiles and antioxidant activity of the SDs developed. The group contribution methods of Hoy and Van Krevelen and Hoftyzer, used for PEG solubility parameter calculations, presented a suitable prediction of interaction and miscibility behaviour. The results suggested the presence of amorphous quercetin precipitates in the crystalline matrix of PEG 4000 and PEG 6000, and the formation of an amorphous SD between quercetin and PEG 1000. These formulations achieved good radical scavenging activity and better dissolution, especially the quercetin-PEG 1000 SDs.