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Although antioxidant therapy holds promise for inflammatory bowel disease (IBD), existing drugs such as natural antioxidants and metal nanozymes cannot meet the requirements for efficacy and/or long-term or even lifelong safety use. We developed a safe and efficient IBD nanomedicine by self-polymerizing natural antioxidant lipoic acid (LA) into conjugated poly(acylic acid) particles (cLAPs). Due to the structural homology with LA monomers, cLAPs exhibit excellent biocompatibility. The cLAPs administered orally selectively attach to the positively charged inflammatory sites in the colon through the negatively charged surface of IBD mice, remaining for over 36 hours. After cell uptake mediated by polydisulfide, cLAPs undergo de-polymerization triggered by glutathione. This process enables the continuous release of reactive oxygen species (ROS) and their retention within the cells for more than 6 hours, providing a possibility for the continuous clearance of ROS, ultimately alleviating intestinal inflammation, restoring the mucosal barrier, and rebalancing the intestinal microbiota. The in vivo results showed that the weight recovery rate of cLAPs-mediated IBD mice was 75.9%, and the colon length recovery rate was 94.4%, with the efficacy being 1.4 times higher than that of the 5-fold higher-dose sulfanilamide (53.3% and 58.3%) and 1.6 times higher than that of the 5-fold higher-dose aminosalicylic acid (53.3% and 58.3%). This natural antioxidant nanomedicine has potential in clinical applications. This research was published in ACS Nano under the title "Natural Antioxidant Lipoic Acid Constructed Nanodrug for Oral Therapy of Inflammatory Bowel Disease".
Reference Information:
DOI: 10.1021/acsnano.5c15530
