Oral Lactoferrin‐Responsive Formulation Anchoring around Inflammatory Bowel Region for IBD Therapy

Oral formulations for inflammatory bowel disease (IBD) are hindered by mucosal damage and diarrhea, limiting drug retention and efficacy. A novel delivery strategy using lactoferrin-responsive flocculation is developed to enhance astaxanthin solubility and safety. This approach improves immunoregulation, epithelial repair, and gut microbiota, leading to increased colon length and 100% survival in vivo, offering a promising method for precise IBD therapy.

Abstract

Oral formulation is the ideal treatment method for inflammatory bowel disease (IBD) therapy, but the mucosal damage and diarrhea symptoms impede the drug retention around the inflammatory region, severely limiting IBD therapeutic efficacy. To address this, an oral astaxanthin (Ast) precise delivery formulation is developed with the selective Ast anchoring around the inflammatory region by the novel lactoferrin (LF)-responsive flocculation. This formulation also heightens the apparent solubility of Ast with the minimized edible safety risks for the edible raw materials. For in vivo IBD therapy, the precise delivery formulation exhibits remarkable outcomes, including a significant increase in colon length and a 100% survival rate. Furthermore, it is verified that the mechanism of treatment is primarily attributed to the improved immunoregulation, epithelial repair, and gut microbiota remodeling after the LF-responsive flocculation. This effective inflammatory-responsive delivery design is instructive and valuable to develop more precise delivery systems for IBD therapy.