PDF(Pubmed)
Abstract：
Quercetin (Q) dietary supplements exhibit poor oral bioavailability because of degradation throughout gastrointestinal digestion (GD), which may be overcome using mesoporous silica particles (MSPs) as an oral delivery system (ODS). This study aimed to elucidate the effect of the functionalization of MSPs with amine-(A-MSP), carboxyl-(C-MSP), or thiol-(T-MSP) groups on their efficiency as a quercetin ODS (QODS). The type and degree of functionalization (DF) were used as factors in an experimental design. The Q-loaded F-MSP (F-MSP/Q) was characterized by gas physisorption analysis, loading capacity (LC), and dynamic light scattering and kinetics of Q release at gastric and intestinal pHs. Antioxidant capacity and Q concentration of media containing F-MSP/Q were evaluated after simulated GD. A-MSP showed the highest LC (19.79 ± 2.42%). C-MSP showed the lowest particle size at pH 1.5 or 7.4 (≈200 nm). T-MSP exhibited the maximum Q release at pH 7.4 (11.43%). High DF of A-MSP increased Q retention, regardless of pH. A-MSP preserved antioxidant capacity of Q-released gastric media (58.95 ± 3.34%). Nonetheless, MSP and F-MSP did not protect antioxidant properties of Q released in intestinal conditions. C-MSP and T-MSP showed essential features for cellular uptake and Q release within cells that need to be assessed.
摘要：
槲皮素（Q）膳食补充剂表现出较差的口服生物利用度，因为整个胃肠道消化（GD）的降解，这可以使用介孔二氧化硅颗粒(MSP)作为口腔递送系统(ODS)来克服。本研究旨在阐明胺（A-MSP）对MSP功能化的影响，羧基-(C-MSP),或巯基（T-MSP）组作为槲皮素ODS（QODS）的效率。功能化（DF）的类型和程度被用作实验设计中的因素。通过气体物理吸附分析表征了负载Q的F-MSP（F-MSP/Q），装载能力(LC)，以及动态光散射和胃和肠pH下Q释放的动力学。模拟GD后评估含F-MSP/Q的培养基的抗氧化能力和Q浓度。A-MSP显示最高LC(19.79±2.42%)。C-MSP在pH1.5或7.4时显示出最低的粒径(约200nm)。T-MSP在pH7.4时表现出最大Q释放(11.43%)。A-MSP的高DF增加了Q保留，不管pH值。A-MSP保留了释放Q的胃介质的抗氧化能力（58.95±3.34％）。尽管如此，MSP和F-MSP不保护在肠道条件下释放的Q的抗氧化性能。C-MSP和T-MSP显示需要评估的细胞内细胞摄取和Q释放的基本特征。
