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Updated: Jun 3, 2025

Non-invasive Assessment of the Efficacy of New Therapeutics for Intestinal Pathologies Using Serial Endoscopic Imaging of Live Mice
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Oral colon-targeted responsive chitosan/pectin-based nanoparticles propels the application of tofacitinib in colitis

Chunfei Wu1,2, Chuanlin Bi3,4, Geun-Soo Kim2

  • 1Medical School, Qingdao Huanghai University, Qingdao, China.

Scientific Reports
|January 10, 2025
PubMed

Insights

New nanoparticles deliver tofacitinib (Tof) directly to the colon, improving ulcerative colitis (UC) treatment by reducing side effects. This targeted approach enhances Tof efficacy for managing moderate to severe UC.

Area of Science:

  • Pharmacology
  • Materials Science
  • Gastroenterology

Background:

  • Tofacitinib (Tof) treats ulcerative colitis (UC) but has dose-dependent systemic side effects.
  • Current treatments necessitate improved drug delivery for enhanced efficacy and reduced toxicity.

Purpose of the Study:

  • To develop an efficient oral colon-targeted drug delivery system for Tof.
  • To construct Tof-loaded nanoparticles (NPs) using pectin, chitosan, bovine serum albumin, and chondroitin sulfate for targeted UC therapy.

Main Methods:

  • Synthesized Tof@BSA-Chs-CP nanoparticles with a pH-sensitive pectin/chitosan shell.
  • Utilized gut microbiota-secreted enzymes to trigger NP degradation in the colon.
  • Evaluated NP performance in mouse colitis models.

Main Results:

  • The pectin/chitosan shell demonstrated pH-sensitive properties, reducing systemic absorption and targeting inflamed colonic sites.
  • Oral administration of Tof@BSA-Chs-CP NPs effectively ameliorated colitis in mice.
  • NP treatment modulated pro-inflammatory cytokines and immune regulatory factors, expediting colitis resolution.

Conclusions:

  • The developed Tof@BSA-Chs-CP NPs show promise for targeted colon delivery of Tof.
  • This targeted delivery system offers a potential strategy to improve Tof therapy for moderate to severe ulcerative colitis while minimizing systemic side effects.
Keywords:
Colon-targeted drug deliveryEnzymatic-triggered releaseUlcerative colitispH-sensitive release

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