School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Food Funct. 2018 Nov 14;9(11):5999-6009. doi: 10.1039/c8fo01216d.
The antioxidant quercetin (Q) is a bioactive compound that can inhibit colon cancer. However, its poor stability in the upper gastro-intestinal tract and low bioavailability compromised its benefits. In this study, a biopolymer-based colon-specific delivery system for Q was constructed by co-axial electrospinning. Quercetin-loaded chitosan nanoparticles (QCNP) were firstly prepared and characterized. Then, a Q-loaded electrospun fiber mat (Q-loaded EFM) containing prebiotics (galactooligosaccharide, GOS) was fabricated using sodium alginate as the shell layer and the abovementioned QCNP and prebiotics as the core layer. The DPPH assay showed that the antioxidant activity of Q was maintained in the obtained film. Owing to the addition of prebiotic GOS, the obtained fiber mat exhibited good prebiotic effects. In vitro release kinetics showed a sustained and targeted colon-specific release of Q from the Q-loaded EFM containing GOS, and the release rate of Q was enhanced by the presence of GOS. The obtained film also exhibited inhibition effects on Caco-2 cells in a dose- and time-dependent manner. Flow cytometry and fluorescence microscopy analysis indicated that the Q-loaded EFM containing GOS exerted its activity on colonic cancer cells by arresting the cell cycle in the G0/G1 phase and triggering apoptotic cell death. This study demonstrates the potential of the obtained film as an oral delivery system for encapsulation, protection, and release of Q at the colon for the oral therapy of colon disorders.
抗氧化剂槲皮素 (Q) 是一种生物活性化合物，可以抑制结肠癌。然而，其在上消化道中的稳定性差和生物利用度低，限制了它的益处。在这项研究中，通过同轴静电纺丝构建了一种基于生物聚合物的结肠特异性递送系统用于 Q。首先制备并表征了载有槲皮素的壳聚糖纳米颗粒 (QCNP)。然后，使用海藻酸钠作为壳层，将上述 QCNP 和益生元（半乳糖寡糖，GOS）作为芯层，制备了含有益生元的载 Q 静电纺纤维毡（载 Q 静电纺纤维毡，Q-loaded EFM）。DPPH 测定表明，所获得的薄膜中 Q 的抗氧化活性得以保持。由于添加了益生元 GOS，所得纤维毡表现出良好的益生元效果。体外释放动力学研究表明，含有 GOS 的载 Q 静电纺纤维毡具有持续的靶向结肠特异性 Q 释放，并且 GOS 的存在增强了 Q 的释放速率。所得薄膜还表现出对 Caco-2 细胞的剂量和时间依赖性抑制作用。流式细胞术和荧光显微镜分析表明，含有 GOS 的载 Q 静电纺纤维毡通过将细胞周期阻滞在 G0/G1 期并触发细胞凋亡来发挥其对结肠癌细胞的作用。这项研究证明了所获得的薄膜作为口服结肠疾病治疗用 Q 包封、保护和释放的口服递送系统的潜力。
