Nanoassemblies Derived from Natural Flavonoid Compounds as New Antioxidant Oral Preparations for Targeted Inflammatory Bowel Disease Therapy

Abstract Possessing the largest surface area of mucosa in the body, the gastrointestinal (GI) tract can easily sufferfrom inflammatory damage under various adverse external exposures, resulting in the occurrence of inflammatory bowel disease (IBD). Excessive reactive oxygen species (ROS) usually lead to local mucosal injury, accelerate the formation of niduses, andamplify the inflammatory and immune response. Antioxidant therapy, therefore, is considered as a potential strategy against IBDs. Herein, a series of novel dihydromyricetin‐based nanoassemblies with excellent antioxidant activities and high dispersion in GI tract as oral preparations are developed for the targeted IBD treatment. By changing raw materials, the current strategy can be well extended to the preparation of other insoluble natural flavonoid compound‐based nanoassemblies. The well‐designed dihydromyricetin‐PEG 1000‐based nanoassemblies (DMY‐1000 NAs) with high stability and great ROS scavenging capacity in the harsh environment of GI tract hold an admirable targeted capability toward the intestinal inflamed lesions. Therefore, these biocompatible DMY‐1000 NAs show promising therapeutic effects for typical IBDs including ulcerative colitis and Crohn's disease in murine models. This study not only provides a new method for constructing antioxidant therapy platforms but also illustrates their prominent therapeutic promise against IBDs.