Despite recent therapeutic advances in the treatment of inflammatory bowel disease (IBD), the off-target systemic side effects of small-molecule drugs or biologics remain problematic. Targeting the site of intestinal inflammation offers an approach to maximize potential therapeutic benefits while minimizing systemic side effects. Importantly, drug combination provides the possibility of tackling IBD through different pathways that could improve the treatment outcome. Here we introduced an inflammation-targeting drug delivery system utilizing albumin-based nanoparticles (NPs) for drug combination with relevance for IBD treatment.