Enhancing the solubility of puerarin via melt sonocrystallization

Abstract

In this work, in order to improve the low solubility and poor oral bioavailability of puerarin, we first applied melt sonocrystallization (MSC) technology to systematically investigate the effects on its solubility and crystallographic properties. We applied MSC to treat puerarin, evaluated its solubilization effect using UV spectroscopy, and characterized it by dissolution rate, optical microscope, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA) and Fourier transform infrared spectroscopy (FTIR). Following MSC treatment, puerarin exhibited higher solubility and faster dissolution, the product displayed reduced particle size and a tendency to agglomerate. The results of PXRD, DSC, FTIR and TGA showed that the crystal form of MSC treated puerarin transformed into puerarin monohydrate, with a decrease in crystallinity and partial amorphization. The reduction in particle size and amorphization may be the driving forces of the increase in solubility and dissolution. In summary, MSC can significantly improve the solubility and dissolution of puerarin, providing new ideas for enhancing its bioavailability and improving its oral formulations.