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

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

  • ACS Nano. 2022 Dec 15. doi: 10.1021/acsnano.2c11188.
Chengke Zhao 1,  Jiali Yang 2,  Mingfeng Chen 1,  Wenjun Chen 1,  Xinyuan Yang 2 3,  Heng Ye 1,  Liying Wang 1,  Yong Wang 1,  Jinjin Shi 2,  Fengxia Yue 4,  Xing Ma 1
Affiliations

Affiliations

  • 1 Sauvage Laboratory for Smart Materials and School of Materials Science and Engineering, Harbin Institute of Technology (Shenzhen), Shenzhen 518055, China.
  • 2 Key Laboratory of Targeting Therapy and Diagnosis for Critical Diseases (Zheng Zhou), School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
  • 3 Institutes of Biomedical Sciences, Fudan University, Shanghai 200032, China.
  • 4 State Key Laboratory of Pulp and Paper Engineering, South China University of Technology, Guangzhou 510640, China.
PMID: 36521055 DOI: 10.1021/acsnano.2c11188
Abstract

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.

Keywords

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

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