Traditional colitis treatment strategies have issues such as side effects and poor lesion targeting. In this study, a milled black rice particle-stabilized Pickering emulsion (BR-5-DMN) has been developed as a delivery vehicle for 5-demethylnobiletin (5-DMN) to treat colitis. The alleviating effects of three 5-DMN delivery systems: BR-5-DMN, Tween 80 emulsion for upper gastrointestinal delivery, and soybean oil with most 5-DMN entering the colon were compared. BR-5-DMN exhibited superior effects, enhancing 5-DMN absorption and metabolic conversion. It also improved intestinal barrier function and microbiome homeostasis, restoring short-chain fatty acid synthesis, especially acetic acid, through releasing dietary fiber, bioactives from black rice, and 5-DMN in the colon. Black rice particles in BR-5-DMN promoted the growth of Bifidobacterium while inhibiting Ruminococcus, and both black rice particles and 5-DMN synergistically increased Akkermansia abundance. This study highlights the potential of milled grain particle-stabilized emulsions as effective vehicles for bioactives to treat colitis by regulating gastrointestinal release and synergistic interactions.
Keywords: 5-demethylnobiletin; Pickering emulsion; colitis; gut microbiota; nano/submicrometer black rice particles.