title: Preparation and characterization of inclusion complexes formed between baicalein and cyclodextrins.
abstract: 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 13672.67l mol(-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 ((1)H NMR), scanning electron microscopy (SEM), and X-ray powder diffractometry (XRPD). The UV-vis, DSC, (1)H 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.
authors: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201210, China.
authors: Qiuna
authors: Q
authors: Zhou
authors: Xiaohui
authors: X
authors: Wei
authors: Wei
authors: W
authors: Dou
authors: Guixin
authors: G
authors: Chou
authors: Zhengtao
authors: Z
authors: Wang
mesh_terms: D003505:Cyclodextrins / Q000737:chemistry*; D044950:Flavanones / Q000737:chemistry*; D005612:Freeze Drying; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry; D012995:Solubility
chemical_list: D003505:Cyclodextrins; D044950:Flavanones; D011108:Polymers; C006680:baicalein