Li Shu-Fang, Hu Teng-Gen, Wu Hong
School of Food Science and Engineering, South China University of Technology, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, Guangzhou 510641, China.
Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences, Key Laboratory of Functional Foods, Ministry of Agriculture, Guangdong Key Laboratory of Agricultural Products Processing, Guangzhou, 510640, China.
Int J Biol Macromol. 2024 Oct;277(Pt 2):134204. doi: 10.1016/j.ijbiomac.2024.134204. Epub 2024 Jul 26.
Quercetin possesses multiple biological activities. To achieve efficient colon-specific release of quercetin, new composite nanofibers were developed by coating pH-responsive shellac on hydrophilic gelatin through coaxial electrospinning. These composite nanofibers contained bead-like structures. The encapsulation efficiency (87.6-98.5 %) and loading capacity (1.4-4.1 %) varied with increasing the initial quercetin addition amount (2.5-7.5 %). FTIR, XRD, and TGA results showed that the quercetin was successfully encapsulated in composite nanofibers in an amorphous state, with interactions occurring among quercetin, gelatin, and shellac. Composite nanofibers had pH-responsive surface wettability due to the shellac coating. In vitro digestion experiments showed that these composite nanofibers were highly stable in the upper gastrointestinal tract, with quercetin release ranging from 4.75 % to 12.54 %. In vivo organ distribution and pharmacokinetic studies demonstrated that quercetin could be sustainably released in the colon after oral administration of composite nanofibers. Besides, the enhanced anticancer activity of composite nanofibers was confirmed against HCT-116 cells by analyzing their effect on cell viability, cell cycle, and apoptosis. Overall, these novel composite nanofibers could deliver efficiently quercetin to the colon and achieve its sustained release, thus potential to regulate colon health. This system is also helpful in delivering other bioactives to the colon and exerting their functional effects.
槲皮素具有多种生物活性。为实现槲皮素在结肠的高效特异性释放，通过同轴静电纺丝将pH响应性虫胶涂覆在亲水性明胶上，制备了新型复合纳米纤维。这些复合纳米纤维含有珠状结构。包封率（87.6 - 98.5%）和载药量（1.4 - 4.1%）随槲皮素初始添加量（2.5 - 7.5%）的增加而变化。傅里叶变换红外光谱（FTIR）、X射线衍射（XRD）和热重分析（TGA）结果表明，槲皮素以无定形状态成功包封在复合纳米纤维中，槲皮素、明胶和虫胶之间存在相互作用。由于虫胶涂层，复合纳米纤维具有pH响应性表面润湿性。体外消化实验表明，这些复合纳米纤维在上消化道中高度稳定，槲皮素释放率为4.75%至12.54%。体内器官分布和药代动力学研究表明，口服复合纳米纤维后，槲皮素可在结肠中持续释放。此外，通过分析复合纳米纤维对HCT - 116细胞活力、细胞周期和凋亡的影响，证实了其增强的抗癌活性。总体而言，这些新型复合纳米纤维能够将槲皮素高效递送至结肠并实现其缓释，因此具有调节结肠健康的潜力。该系统也有助于将其他生物活性物质递送至结肠并发挥其功能作用。
