Solubility and dissolution enhancement of quercetin Via preparation of spray dried microstructured solid dispersions

Abstract

Quercetin (QC) is a bioflavonoid characterized with poor water solubility that limits its oral bioavailability and hence its therapeutic applications. In an attempt to enhance its solubility and dissolution rate, both binary and ternary microstructured solid dispersions (MSDs) of QC with different ratios of polyvinylpyrrolidone K30 (PVP K30) and pluronic F 127 (PF 127) were prepared by spray drying. Solubility and dissolution characteristics of the prepared solid dispersions were evaluated and compared with that of the corresponding physical mixtures and the drug powder. The obtained results revealed that the solubility and the dissolution rate of QC were greatly improved in binary microstructured solid dispersions (MBSD), as well as in ternary microstructured solid dispersions (MTSD). MTSD, made up of 5% w/w PF 127, and 95% w/w QC/PVP K30 in 1:1 weight ratio, showed enhanced QC solubility and dissolution. The percent of QC dissolved after 60 minutes (%D60min) was 95.1, and the time required for 90% of QC to be dissolved (T90%) was 50 minutes Physical characterization of MTSD by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD), in comparison with corresponding physical mixtures, revealed changes in solid state of QC during the formation of solid dispersion that indicate the formation of high-energy amorphous phase.