Si Yanxue, Cha Ruitao, Zhang Pai, Zhou Fengshan, Yuan Wenbing, Jiang Xingyu
Beijing Key Laboratory of Materials Utilization of Nonmetallic Minerals and Solid Wastes, National Laboratory of Mineral Materials, School of Materials Science and Technology, China University of Geosciences (Beijing), Beijing, 100083, P. R. China.
Laboratory of Theoretical and Computational Nanoscience, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology, Beijing, 100190, P. R. China.
Adv Healthc Mater. 2025 Aug;14(22):e2501160. doi: 10.1002/adhm.202501160. Epub 2025 Jun 23.
5-Aminosalicylic acid (5-ASA) is the first-line drug for ulcerative colitis (UC), which encounters therapeutic constraints due to the poor water solubility and absorption by the upper gastrointestinal. Here, a cyclodextrin-based metal-organic framework (CD-MOF) is used as a carrier for 5-ASA (ASA@CM) to enhance its solubility. To improve the targeted release 5-ASA, ASA@CM is incorporated into sodium alginate/L-arginine complex (SA-LA) to obtain the desired microspheres (ASA@CM/SL) by electrospray. ASA@CM/SL safeguards 5-ASA against the harsh gastrointestinal environment and provides favorable delivery to the colon. The anti-inflammatory and anti-oxidant activity is studied by measuring inflammatory factors and reactive oxygen species (ROS). The therapeutic effect of ASA@CM/SL on UC mice induced with dextran sulfate sodium is assessed. The biosafety by evaluating cytotoxicity and organ toxicity is studied. ASA@CM/SL shows excellent therapeutic effects for UC, as evidenced by its alleviation of inflammatory response and restoration of disrupted intestinal barriers. ASA@CM/SL features low cytotoxicity and low organ toxicity. This study provides a potential strategy for improving 5-ASA solubility and delivery efficiency, which may also be applied to broadly tackle various small hydrophobic molecules to treat UC and other intestinal diseases.
