Ulcerative colitis is a severe chronic inflammatory bowel disease characterized by intestinal barrier dysfunction, immune dysregulation, and microbial dysbiosis. Although plant-derived bioactive compounds exhibit anti-inflammatory, antioxidant, and barrier-repairing potential, their oral bioavailability and targeted efficacy remain limited, necessitating advanced delivery strategies to enhance therapeutic outcomes. The spatiotemporal advantages of targeted and synergistic delivery systems in modulating the release kinetics, biological transport pathways, and mechanistic actions of bioactive compounds within the gastrointestinal tract were highlighted. By integrating pH-responsive, enzyme-triggered, and microbiota-activated materials with technologies such as sustained/controlled release, hierarchical structuring, mucosal permeation enhancement, and ligand-modified targeting, site-specific release, local enrichment, and synergistic effects of bioactive compounds were achieved by these systems. The localized concentration and duration of bioactives in the small intestine or colon were significantly improved, amplifying their ability to regulate immune-inflammatory networks, restore mucosal barriers, and remodel the microbiota-metabolite axis. Furthermore, synergistic regulatory mechanisms at the systemic level, including portal vein-lymphatic absorption ratios, microbiota-dependent metabolic conversion ratios, and circadian rhythm-responsive signaling were explored. Targeted delivery systems are not merely delivery vehicles, but also represent a precision intervention platform that orchestrates the biological fate and multi-target effects of functional ingredients. These advancements provided a systematic theoretical foundation and technological framework for functional food-based interventions in chronic inflammatory diseases such as colitis. 〖