Department of Food Science and Technology, School of Nutrition and Food Science, Isfahan University of Medical Sciences, Isfahan, Iran.
Food Security Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
Int J Nanomedicine. 2019 Jun 24;14:4589-4599. doi: 10.2147/IJN.S206350. eCollection 2019.
Ferulic acid (FA) is a poorly water-soluble natural antioxidant with anticancer activity. This poor solubility limits the application of FA in the food and pharmaceutical industry. Cyclodextrin nanosponges (CD-NSs) are a novel group of cross-linked CD derivatives which can be used to enhance the solubility of low-soluble bioactive compounds. In this study, FA was encapsulated into the NSs in the proportion of 1:4 (FA:NS). Diphenyl carbonate was used as a cross-linker in different proportions with β-CD. Characterization of obtained NSs was performed using scanning electron microscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis. Our results revealed that the solubility of encapsulated FA was increased up to fifteenfold compared with pure FA in the proportion of 1:4 (CD:cross-linker). The results of FTIR, XRD, and DSC confirmed the interaction of FA with NSs. The cytotoxicity of encapsulated FA against MCF7 and 4T1 breast cancer cell lines was investigated using different concentrations of FA in 24, 48, and 72 hrs. The cytotoxicity assay indicated that FA treatment reduced viability and enhanced apoptosis of cancer cells. IC50 value of encapsulated FA (250 ppm) was decreased by threefold when compared with pure FA (750 ppm). In general, CD-NS was found to be a suitable delivery system for poorly soluble bioactives such as FA.
阿魏酸（FA）是一种水溶性较差的天然抗氧化剂，具有抗癌活性。这种较差的溶解度限制了 FA 在食品和制药工业中的应用。环糊精纳米海绵（CD-NSs）是一类新型交联 CD 衍生物，可用于提高低溶解度生物活性化合物的溶解度。在这项研究中，FA 以 1:4（FA:NS）的比例被包封到 NS 中。碳酸二苯酯以不同比例与β-CD 一起用作交联剂。通过扫描电子显微镜、X 射线衍射（XRD）、差示扫描量热法（DSC）和傅里叶变换红外（FTIR）分析对获得的 NS 进行了表征。我们的结果表明，与纯 FA 相比，以 1:4（CD:交联剂）的比例包封的 FA 的溶解度增加了十五倍。FTIR、XRD 和 DSC 的结果证实了 FA 与 NSs 的相互作用。使用不同浓度的 FA 在 24、48 和 72 小时研究了包封 FA 对 MCF7 和 4T1 乳腺癌细胞系的细胞毒性。细胞毒性测定表明，FA 处理降低了癌细胞的活力并增强了细胞凋亡。与纯 FA（750 ppm）相比，包封 FA（250 ppm）的 IC50 值降低了三倍。总的来说，CD-NS 被发现是一种适合包封疏水性生物活性物质（如 FA）的递送系统。
