Oral co-delivery of nutraceuticals at colon sites has been considered the preferable strategy for targeted ulcerative colitis(UC)relief.This study aimed to develop oral colon-targeting nanoparticles(NPs)co-loaded with...Oral co-delivery of nutraceuticals at colon sites has been considered the preferable strategy for targeted ulcerative colitis(UC)relief.This study aimed to develop oral colon-targeting nanoparticles(NPs)co-loaded with egg white-derived peptides(EWDP)and hydrophobic quercetin(Que)using Zein/chondroitin sulfate(CS)templates.The fabricated NPs showed excellent pH-sensitive size tunability(488.0-128.6 nm)and Que co-encapsulation efficiency(99.3%,pH 7.0),owing to the EWDP co-assembly with templates driven by three main noncovalent interactions(hydrogen bonding,electrostatic and hydrophobic interaction).Notably,the less active EWDP could act as the promising co-assembly enhancers and excipient analogs to sufficiently exert the preferable oral synergism(e.g.,antioxidant and anti-inflammatory)of the two nutraceuticals,mainly through enhancing its aqueous solubility,controlled release,and transport stability of Que(>20%)under gastrointestinal conditions.Moreover,EWDP could jointly co-assembly with active targeting biopolymers(e.g.,CS)to induce the superior colon-targeted accumulation of NPs,thereby dramatically repairing intestinal barriers(tight junction and mucus layer)and restoring gut microbiota balance(e.g.,enriching Lachnospiraceae and eliminating Bacteroidota).Overall,this study provides a facile and efficient orally colon-targeted nano-strategy for multiple nutraceuticals in precise UC mitigation.Meanwhile,the co-assembly profiles of EWDP could offer an insightful and widely applicable insight into the ingenious formulation of biopolymer nanoplatforms(active targeting or passive targeting)in food processing and healthcare areas.展开更多
基金funded by the National Key R&D Program of China(2022YFD2101002)China Postdoctoral Science Foundation(2024M761133&2024M751093&GZB20230261&2023TQ0130)Jilin University Innovative Training Program for College Students(202410183189).
文摘Oral co-delivery of nutraceuticals at colon sites has been considered the preferable strategy for targeted ulcerative colitis(UC)relief.This study aimed to develop oral colon-targeting nanoparticles(NPs)co-loaded with egg white-derived peptides(EWDP)and hydrophobic quercetin(Que)using Zein/chondroitin sulfate(CS)templates.The fabricated NPs showed excellent pH-sensitive size tunability(488.0-128.6 nm)and Que co-encapsulation efficiency(99.3%,pH 7.0),owing to the EWDP co-assembly with templates driven by three main noncovalent interactions(hydrogen bonding,electrostatic and hydrophobic interaction).Notably,the less active EWDP could act as the promising co-assembly enhancers and excipient analogs to sufficiently exert the preferable oral synergism(e.g.,antioxidant and anti-inflammatory)of the two nutraceuticals,mainly through enhancing its aqueous solubility,controlled release,and transport stability of Que(>20%)under gastrointestinal conditions.Moreover,EWDP could jointly co-assembly with active targeting biopolymers(e.g.,CS)to induce the superior colon-targeted accumulation of NPs,thereby dramatically repairing intestinal barriers(tight junction and mucus layer)and restoring gut microbiota balance(e.g.,enriching Lachnospiraceae and eliminating Bacteroidota).Overall,this study provides a facile and efficient orally colon-targeted nano-strategy for multiple nutraceuticals in precise UC mitigation.Meanwhile,the co-assembly profiles of EWDP could offer an insightful and widely applicable insight into the ingenious formulation of biopolymer nanoplatforms(active targeting or passive targeting)in food processing and healthcare areas.
