Li Dan, Yi Gaoyang, Cao Guifang, Midgley Adam C, Yang Yongli, Yang Dan, Liu Wenguang, He Yujuan, Yao Xiaolin, Li Guoliang
School of Food and Biological Engineering, Shaanxi University of Science and Technology, Xi'an, Shaanxi, 710021, P. R. China.
Key Laboratory of Bioactive Materials for the Ministry of Education, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
Small. 2025 Apr;21(16):e2410124. doi: 10.1002/smll.202410124. Epub 2025 Mar 13.
The utilization of plant-derived exosome-like nanovesicles (ELNs) as nanocarriers for oral delivery of bioactives has garnered significant attention. However, their distinctive lipid membrane composition may result in elevated membrane permeability within the gastrointestinal environment, leading to the leakage of carried bioactives. Inspired by the concept of projectile design, Tartary buckwheat-derived ELNs (TB-ELNs) based dual-carriers are fabricated by loading chlorogenic acid (CGA) into the cores and bonding selenium nanoparticles (SeNPs) to the lipid membrane. The results indicate that SeNPs bond markedly augments the membrane rigidity, and therefore enhances the stability of TB-ELNs and the retention rate of the loaded CGA during gastrointestinal digestion. In vitro and in vivo studies indicates that the TB-ELNs based dual-carriers are internalized by epithelial cells and transcytosis via the endoplasmic reticulum, and show the synergistic regulatory effect on high-fat diet-induced hyperglycemia in the intestine-liver axis. These results may be attributed to the fact that SeNPs combination reduces the gastrointestinal degradation of the carried bioactives. Moreover, SeNPs with antioxidant property can protect ELNs and their carried bioactives from oxidative damage, thereby enhancing their biological activities. Collectively, this study offers a new strategy to develop highly efficient oral delivery systems for bioactives to alleviate hyperglycemia and diabetes.
利用植物来源的类外泌体纳米囊泡（ELNs）作为生物活性物质口服递送的纳米载体已引起广泛关注。然而，其独特的脂质膜组成可能导致在胃肠道环境中膜通透性升高，从而导致所载生物活性物质泄漏。受抛射体设计概念的启发，通过将绿原酸（CGA）负载到核心中并将硒纳米颗粒（SeNPs）结合到脂质膜上，制备了基于苦荞来源的ELNs（TB-ELNs）的双载体。结果表明，SeNPs的结合显著增强了膜的刚性，从而提高了TB-ELNs的稳定性以及在胃肠道消化过程中所载CGA的保留率。体外和体内研究表明，基于TB-ELNs的双载体被上皮细胞内化并通过内质网进行转胞吞作用，并在肠-肝轴上对高脂饮食诱导的高血糖症显示出协同调节作用。这些结果可能归因于SeNPs组合减少了所载生物活性物质的胃肠道降解。此外，具有抗氧化特性的SeNPs可以保护ELNs及其所载生物活性物质免受氧化损伤，从而增强它们的生物活性。总的来说，这项研究为开发高效的生物活性物质口服递送系统以缓解高血糖和糖尿病提供了一种新策略。
