Utilizing spray drying technique to improve oral bioavailability of apigenin

摘要

The aim of this study was to prepare, characterize, and evaluate apigenin in a solid dispersion system to improve the dissolution rate and bioavailability of such poorly soluble drug. Apigenin was dissolved in organic solvent with micelle forming polymer Pluronic F-127 (PL-F127). Solid dispersion of apigenin-PL F-127 was developed using spray drying technique. Physicochemical and in vitro characterization of the produced solid dispersion particles were conducted using scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffractometry and dissolution study. In addition, in vivo study was performed for the spray dried versus pure and marketed apigenin. C-max was found to be around 5 folds higher for spray dried product compared to non spray dried materials. The prepared drug: polymer formulation showed elongated particles and complete lack of crystallinity at 1: 4 ratio. The change in the vibrational wave numbers strongly suggested the formation of hydrogen bonding between apigenin and PL F-127. Significant increase in the dissolution rate and bioavailability of the spray dried apigenin showed the potential of solid dispersion system to overcome problem related to BCS II drugs. (C) 2018 The Society of Powder Technology Japan. Published by Elsevier B.V. and The Society of Powder Technology Japan. All rights reserved.