Pellets containing quercetin amino acid co-amorphous mixture for the treatment of pain: Formulation, optimization, in-vitro and in-vivo study

Abstract

Quercetin (QCT) shows many therapeutic applications but is constrained to its oral use due to its low bioavailability. In this study, co-amorphous mixture QCT with different amino acids (Arginine, Glutamic acid, Aspartic acid, Tryptophan, and Glycin) of different molar ratios was prepared using ball milling method. The solubility and physicochemical study of the mixtures was done using FTIR and XRD study. The co-amorphous mixtures QCT: ARG (1:2) was formulated in pellets using extrusion spheronization method. In-vitro dissolution study F1 formulation showed (95.74 ± 4.58%) significant increase (P < 0.005) compared to the pure drug (21.85 ± 3.42%) and other formulations. The in-vivo study F1 showed a significant (p < 0.05) increases in percent inhibition (67.00%) compared to pure drug (31%). The F1 formulation was stable when subjected to stability study. Therefore, the prepared co-amorphous mixture loaded pellets enhance the solubility, bioavailability, and stability of quercetin.