Inclusion complex of barbigerone with hydroxypropyl-β-cyclodextrin: preparation and in vitro evaluation.

The aim of this study was to improve the water solubility of barbigerone by complexing it with hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexation behavior, characterization and interactions of barbigerone with HP-β-CD were investigated in both solution and the solid state by means of UV/VIS, (1)H NMR, FT-IR, PXRD, SEM. All the characterization information demonstrated the formation of barbigerone-HP-β-CD (bar-HP-β-CD) inclusion complex, and the bar-HP-β-CD inclusion compounds exhibited different spectroscopic features and properties from barbigerone. The results demonstrated that the water solubility of barbigerone was notably increased in the presence of HP-β-CD. Furthermore, preliminary in vitro cytotoxicity assay showed that bar-HP-β-CD still maintain the anticancer activity of barbigerone. These results suggest that HP-β-CD will be potentially useful in the delivery of water-insoluble anticancer agents such as barbigerone.