Lauro Maria Rosaria, Crascí Lucia, Sansone Francesca, Cardile Venera, Panico Anna Maria, Puglisi Giovanni
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084 Fisciano, Italy.
Department of Drug Science, University of Catania, Viale A. Doria, 95100 Catania, Italy.
Oxid Med Cell Longev. 2017;2017:7503240. doi: 10.1155/2017/7503240. Epub 2017 Mar 7.
The aim of this study was to evaluate the antidegenerative effect in osteoarthritis damage of eriocitrin alone and eriocitrin formulated as innovative "dietary flavonoid supplement." A complexation between eriocitrin and hydroxypropyl -cyclodextrin by solubilization/freeze-drying method was performed. The complex in solution was evaluated by phase solubility studies and the optimal 1 : 2 flavanone/cyclodextrin molar ratio was selected. Hydroxypropyl -cyclodextrin was able to complex eriocitrin as confirmed by UV-Vis absorption, DSC, and FTIR studies. The complex formed increased the eriocitrin water solubility (from 4.1 ± 0.2 g·L to 11.0 ± 0.1 g·L) and dissolution rate (from 37.0% to 100%) in 30 min. The in vitro studies exhibit the notion that eriocitrin and its complex inhibit AGEs in a similar manner because hydroxypropyl -cyclodextrin does not interfere with the flavanone intrinsic property. Instead, the presence of cyclodextrin improves eriocitrin antioxidant stability maintaining a high fluorescence value until 8 hours with respect to the pure materials. Moreover, hydroxypropyl -cyclodextrin showed moderate GAGs restoration acting synergistically with the complexed compound to maintain the structural chondrocytes integrity. The results point out that ERT/HP-betaCD complex possesses technological and biological characteristics able to obtain an easily soluble nutraceutical product, which reduces the degenerative and oxidative damage which occurs in osteoarthritis, and improve the patient compliance.
本研究的目的是评估橙皮苷单独使用以及制成创新型“膳食类黄酮补充剂”形式的橙皮苷对骨关节炎损伤的抗退变作用。通过溶解/冷冻干燥法使橙皮苷与羟丙基-β-环糊精形成络合物。通过相溶解度研究对溶液中的络合物进行评估，并选择了最佳的1∶2黄烷酮/环糊精摩尔比。紫外-可见吸收光谱、差示扫描量热法和傅里叶变换红外光谱研究证实，羟丙基-β-环糊精能够与橙皮苷形成络合物。形成的络合物使橙皮苷的水溶性在30分钟内从4.1±0.2 g·L提高到11.0±0.1 g·L，溶解速率从37.0%提高到100%。体外研究表明，橙皮苷及其络合物以相似的方式抑制晚期糖基化终末产物，因为羟丙基-β-环糊精不会干扰黄烷酮的固有特性。相反，环糊精的存在提高了橙皮苷的抗氧化稳定性，相对于纯物质而言，在8小时内保持较高的荧光值。此外，羟丙基-β-环糊精表现出适度的糖胺聚糖恢复作用，与络合化合物协同作用以维持软骨细胞的结构完整性。结果表明，橙皮苷/羟丙基-β-环糊精络合物具有技术和生物学特性，能够获得一种易溶性营养产品，该产品可减少骨关节炎中发生的退变和氧化损伤，并提高患者的依从性。
