Investigation of in vivo efficacy of colon targeted nano-drug delivery systems in TNBS-induced colitis rat model for inflammatory bowel disease


TURANLİ Y., Emniyet Sert A. A., DEMİREL M. A., ÖZKAN Y., Kaplanoğlu G. T., Acartürk F.

Journal of Drug Delivery Science and Technology, cilt.120, 2026 (SCI-Expanded, Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 120
  • Basım Tarihi: 2026
  • Doi Numarası: 10.1016/j.jddst.2026.108260
  • Dergi Adı: Journal of Drug Delivery Science and Technology
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, EMBASE
  • Anahtar Kelimeler: Budesonide, Colon targeting, Controlled release, Crohn's disease, Nano-drug delivery, Ulcerative colitis
  • Gazi Üniversitesi Adresli: Evet

Özet

Inflammatory bowel disease (IBD), which can be classified into Crohn's disease and ulcerative colitis, is a chronic illness characterized by inflammation of the gastrointestinal system (GIS). IBD is typically treated with pH-sensitive drug delivery systems. However, the use of solely pH-dependent drug delivery systems are generally ineffective due to changes in intestinal pH. To overcome the insufficiency of them, we developed budesonide-loaded pH- and time-dependent nano-drug delivery systems for the treatment of IBD and investigated in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis rats in this study. Drug release studies were carried out at pH 1.2, 6.8, and 7.4. The indicators of inflammation in the colonic tissue, like tumor necrosis factor-alpha (TNF-α), Interleukin (IL)-10, and myeloperoxidase (MPO) levels were investigated. In addition, the distribution of nano-drug delivery systems in various parts of the rat gastrointestinal system and the histological evaluation were performed. The NP3 (90% Eudragit S100,10% Eudragit RL100) nanoparticle and NF3 (95% Eudragit S100, 5% Eudragit RL100) nanofiber formulations indicated the most suitable drug release as a colon-specific drug delivery system with a minor release at pH 1.2, 6.8, and major release at pH 7.4. Based on stability studies, it was observed that the formulations, due to the advantage of being in solid form, maintained their physicochemical structure and release profiles when stored under appropriate conditions. Budesonide-loaded nanofibers and nanoparticles improved the TNBS-induced colitis. Treatment with nano-drug delivery systems decreased the damage score. Inflammatory parameters associated with colonic histologic damage were significantly reduced. Drug distribution studies through the gastrointestinal tract monitored with fluorescence microscopy revealed that NF3 and NP3 achieved better colon-specific distribution. Based on the experiments and histological results, budesonide-loaded nano-drug delivery systems appear to be a promising option for treating IBD.