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Carbohydr Polym. 2014 Jan 30;101:623-30. doi: 10.1016/j.carbpol.2013.09.035. Epub 2013 Sep 23.

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

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State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, PR China; Department of Bio-pharmaceutical Engineering, School of Chemical Engineering, Sichuan University, Chengdu 610065, PR China; College of Materials and Chemistry and Chemical Engineering, Chengdu University of Technology, Chengdu 610059, PR China.


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.


Anti-cancer; Barbigerone; Characterization; Hydroxypropyl-β-cyclodextrin; Inclusion complex; Solubility

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