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首页> 外文期刊>RSC Advances >Synthesis and controlled curcumin supramolecular complex release from pH-sensitive modified gum-arabic-based hydrogels
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Synthesis and controlled curcumin supramolecular complex release from pH-sensitive modified gum-arabic-based hydrogels

机译：pH敏感的改性阿拉伯树胶基水凝胶的合成和姜黄素超分子复合物的释放

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Curcumin (CUR) is a polyphenolic compound including a beta-diketone moiety, which is associated with numerous pharmacological activities, but applications are limited due to its low water solubility. Thus, in this work some inclusion complexes of CUR with alpha-cyclodextrin (alpha-CD) and beta-cyclodextrin (beta-CD) were prepared using different host : guest proportions to improve drug solubilization in biological fluids. The formation of these complexes was confirmed by H-1 NMR and thermogravimetric analysis. The stoichiometries of the CUR/alpha-CD and CUR/beta-CD complexes were 1 : 1 and 1 : 2 and the association constants were 344 mol(-1) L and 7.2 x 10(7) mol(-2) L-2 for alpha-CD and beta-CD, respectively. The major stability of the CUR/beta-CD complex is justified by an inclusion of the aromatic ring inside the CD cavity, whilst in the case of alpha-CD-complexes the interactions occur via H-bridges, showing the latter complexes' slow exchange on the NMR time-scale. Even so, the solubility of curcumin complexes is clearly controlled by the solubility of CDs, showing the highest solubility for CUR/alpha-CD complexes. Hydrogels of modified gum arabic containing CUR/alpha-CD (1 : 4) were obtained and used for controlled release of CUR in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF). The kinetics of release was pH-responsive and the percentage of CUR released was ca. 97% in SIF and 6.7% in SGF. For the toxicity studies on undifferentiated Caco-2 cells, IC(50)s of 63.4 +/- 14.4 mu g mL(-1) and 85.2 +/- 14.9 mu g mL(-1) for CUR and CUR/alpha-CD (1 : 4), respectively, were obtained. The toxicity of these samples on differentiated Caco-2 cells was lower than on undifferentiated cells. Additionally, the CUR incorporated into hydrogels showed no toxic effects on differentiated and undifferentiated Caco-2 cells, indicating the pharmaceutical potential of three-dimensional matrices of GAm for controlled release of CUR complexed with cyclodextrin.
机译：姜黄素（CUR）是一种包含β-二酮部分的多酚化合物，与多种药理活性有关，但由于其水溶性低，因此应用受到限制。因此，在这项工作中，使用不同的宿主：客体比例制备了CUR与α-环糊精（α-CD）和β-环糊精（β-CD）的包合物，以改善药物在生物流体中的溶解度。通过H-1 NMR和热重分析证实了这些络合物的形成。 CUR /α-CD和CUR /β-CD复合物的化学计量比为1：1和1：1：2，缔合常数为344 mol（-1）L和7.2 x 10（7）mol（-2）L- 2个分别用于alpha-CD和beta-CD。 CUR /β-CD复合物的主要稳定性是通过在CD腔内包含芳环来证明的，而在α-CD复合物的情况下，相互作用是通过H桥发生的，这表明后者的交换缓慢在NMR时标上。即便如此，姜黄素复合物的溶解度仍由CD的溶解度明确控制，显示出对CUR /α-CD复合物的最高溶解度。获得了含有CUR /α-CD（1：4）的阿拉伯胶改性水凝胶，并将其用于在模拟肠液（SIF）和模拟胃液（SGF）中控制CUR的释放。释放的动力学是pH响应的，并且释放的CUR的百分比为约。 SIF为97％，SGF为6.7％。对于未分化的Caco-2细胞的毒性研究，对于CUR和CUR / alpha-CD，IC（50）分别为63.4 +/- 14.4μg mL（-1）和85.2 +/- 14.9μg mL（-1）获得了（1∶4）。这些样品对分化的Caco-2细胞的毒性低于未分化的细胞。另外，掺入水凝胶中的CUR对分化和未分化的Caco-2细胞没有毒性作用，表明GAm三维矩阵对与环糊精复合的CUR的控制释放具有潜在的药用潜力。

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