Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Drug Dev Ind Pharm. 2011 Aug;37(8):886-93. doi: 10.3109/03639045.2010.548066. Epub 2011 Jan 20.
To evaluate the effect of different cyclodextrins (β-cyclodextrin [β-CD], methyl-β-cyclodextrin [Mβ-CD], or hydroxypropyl-β-cyclodextrin [HPβ-CD]) and/or hydrophilic polymers (carboxymethylcellulose, hydroxypropylmethylcellulose [HPMC], polyethyleneglycol, or polyvinylpyrrolidone [PVP]) on daidzein solubility in water.
The corresponding associations were characterized in aqueous media using phase-solubility studies. The morphology of daidzein/cyclodextrin freeze-dried complexes was characterized using scanning electron microscopy, and their spatial configuration was proposed by means of nuclear magnetic resonance spectroscopy.
In the presence of 6 mM of cyclodextrins, the solubility of daidzein in water was significantly enhanced: 5.7-fold (β-CD), 7.2-fold (Mβ-CD), and 9.4-fold (HPβ-CD). The analysis of the three solid complexes proved that the formation of inclusion complexes occurred through the insertion of the B and C rings of daidzein molecule into the cyclodextrins cavity. The association of daidzein/cyclodextrin complexes to the hydrophilic polymers HPMC or PVP (1%, w/w) was able to improve the solubility of daidzein even further.
The highest solubilizing effect was obtained for daidzein/HPβ-CD/PVP ternary system (12.7-fold).
评估不同环糊精（β-环糊精[β-CD]、甲基-β-环糊精[Mβ-CD]或羟丙基-β-环糊精[HPβ-CD]）和/或亲水性聚合物（羧甲基纤维素、羟丙基甲基纤维素[HPMC]、聚乙二醇或聚乙烯吡咯烷酮[PVP]）对大豆苷元在水中溶解度的影响。
在水介质中通过相溶解度研究对相应的配合物进行了表征。使用扫描电子显微镜对大豆苷元/环糊精冷冻干燥复合物的形态进行了表征，并通过核磁共振波谱法提出了它们的空间构型。
在 6mM 环糊精存在的情况下，大豆苷元在水中的溶解度显著提高：提高了 5.7 倍（β-CD）、7.2 倍（Mβ-CD）和 9.4 倍（HPβ-CD）。对三种固体配合物的分析证明，包合复合物的形成是通过将大豆苷元分子的 B 和 C 环插入环糊精空腔中发生的。将大豆苷元/环糊精复合物与亲水性聚合物 HPMC 或 PVP（1%，w/w）结合能够进一步提高大豆苷元的溶解度。
大豆苷元/HPβ-CD/PVP 三元体系的增溶效果最高（提高了 12.7 倍）。
