4.8 Article

Synthetic Lignin-Derived Therapeutic Nano Reagent as Intestinal pH-Sensitive Drug Carriers Capable of Bypassing the Gastric Acid Environment for Colitis Treatment

Journal

ACS NANO
Volume 17, Issue 1, Pages 811-824

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsnano.2c11188

Keywords

lignin; inflammatory bowel disease; nanoparticle; self-assembly; reactive oxygen species; drug delivery; synergistic therapy

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This study introduces a therapeutic nano reagent, FALNP, which has favorable antioxidant activity and can be orally administered to treat inflammatory bowel disease. The pH-responsive degradability of FALNP allows it to withstand the harsh gastric acid environment, bypass physiological barriers, and target the intestine for gastrointestinal delivery. In vivo experiments showed that FALNP relieved pathological symptoms of acute colitis by reducing oxidative stress and regulating the gut microbiome.
Oral drug delivery is a common route for management of inflammatory bowel disease (IBD) but suffers from low bioavailability and systemic side effects during passage through the alimentary canal. Here, we present a therapeutic nano reagent of a ferulic acid-derived lignin nanoparticle (FALNP). We showed that FALNP with favorable antioxidant activity can regulate IBD. More importantly, the intestinal pH -responsive degradability of FALNP allows it to withstand the harsh gastric acid environment, bypass physiological barriers, and target the intestine for gastrointestinal delivery. In vivo experiments showed that oral administration of FALNP markedly relieved pathological symptoms in a mouse model of acute colitis by reducing oxidative stress and regulating the gut microbiome. By integrating anti-inflammatory medicine, FALNP also can be used as a bioactive carrier to exert a potent synergistic therapeutic effect. In addition to colitis, FALNP can be readily adaptable for use as a carrier platform for therapy of many other intestinal diseases.

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