Preparation and characterization of inclusion complexes formed between baicalein and cyclodextrins

Zhou, Qiuna; Wei, Xiaohui; Dou, Wei; Chou, Guixin; Wang, Zhengtao

Preparation and characterization of inclusion complexes formed between baicalein and cyclodextrins

2013

Zhou, Qiuna | Wei, Xiaohui | Dou, Wei | Chou, Guixin | Wang, Zhengtao

This study investigates the solubility of baicalein (Ba) with the addition of modified cyclodextrins using phase solubility method. The solubility of Ba in the presence of natural (α-, β-, and γ-) cyclodextrins and its derivatives, namely, hydroxypropyl-β-cyclodextrin (HP-β-CD) and (2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD), was higher than that of free Ba. In particular, the stability constant of inclusion complex with DM-β-CD was 13672.67lmol−1, which was the highest among the examined cyclodextrins. The inclusion complexes of Ba and DM-β-CD were prepared via freeze-drying method, which were both characterized in the solution and solid state by UV–vis spectroscopy, differential scanning calorimetry (DSC), proton nuclear magnetic resonance (1H NMR), scanning electron microscopy (SEM), and X-ray powder diffractometry (XRPD). The UV–vis, DSC, 1H NMR, SEM, and XRPD results proved the formation of inclusion complex between Ba and DM-β-CD. Furthermore, the dissolution rate and thermal stability of the inclusion complex were significantly enhanced compared with the pure drug. Therefore, using DM-β-CD can effectively improve the solubility and thermal stability of free Ba, which is a promising approach to promote its clinical application.

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