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Background <p>Irritable bowel syndrome (IBS) requires long-term, site-specific therapy. Mebeverine hydrochloride is effective but limited by rapid metabolism and frequent dosing. This study aimed to develop colon-targeted, controlled-release nanoparticles to improve therapeutic efficacy and compliance.</p> Methods <p>Nanoparticles were prepared via chitosan–xanthan gum polyelectrolyte complexation and optimized using a Box–Behnken design. Molecular docking predicted strong binding of mebeverine to the muscarinic acetylcholine receptor (–7.4&#xa0;kcal/mol). Optimized nanoparticles were enteric-coated with Eudragit S100 for pH-dependent colonic release and evaluated through in vitro dissolution and in vivo efficacy in an acetic acid-induced IBS-D rat model.</p> Results <p>Optimized nanoparticles showed a mean size of ~ 380&#xa0;nm, zeta potential + 25 mV, and entrapment efficiency of 95%. In vitro, the enteric-coated formulation resisted gastric pH and released &gt; 95% drug under colonic conditions within 12&#xa0;h. In vivo, treated rats demonstrated significantly reduced visceral hypersensitivity (AWR score, <i>p</i> &lt; 0.05), normalized intestinal motility (<i>p</i> &lt; 0.05), and improved behavioral outcomes compared to the IBS group. High-dose nanoparticles performed better than the marketed sustained-release capsule.</p> Conclusion <p>The chitosan–xanthan gum nanoparticle system enabled sustained, colon-specific delivery of mebeverine hydrochloride with superior therapeutic efficacy in vivo, offering a promising strategy for long-term IBS management.</p> Graphical abstract <p></p>

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Development and evaluation of chitosan–xanthan gum-based controlled release nanoparticles of mebeverine hydrochloride for targeted IBS therapy: in silico, in vitro, and in vivo investigations

  • 期刊论文

  • 发表日期：

    2025年12月27日

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  • V V Siva Krishna Pushadapu,
  • Grandhi Srikar

摘要

Background

Irritable bowel syndrome (IBS) requires long-term, site-specific therapy. Mebeverine hydrochloride is effective but limited by rapid metabolism and frequent dosing. This study aimed to develop colon-targeted, controlled-release nanoparticles to improve therapeutic efficacy and compliance.

Methods

Nanoparticles were prepared via chitosan–xanthan gum polyelectrolyte complexation and optimized using a Box–Behnken design. Molecular docking predicted strong binding of mebeverine to the muscarinic acetylcholine receptor (–7.4 kcal/mol). Optimized nanoparticles were enteric-coated with Eudragit S100 for pH-dependent colonic release and evaluated through in vitro dissolution and in vivo efficacy in an acetic acid-induced IBS-D rat model.

Results

Optimized nanoparticles showed a mean size of ~ 380 nm, zeta potential + 25 mV, and entrapment efficiency of 95%. In vitro, the enteric-coated formulation resisted gastric pH and released > 95% drug under colonic conditions within 12 h. In vivo, treated rats demonstrated significantly reduced visceral hypersensitivity (AWR score, p < 0.05), normalized intestinal motility (p < 0.05), and improved behavioral outcomes compared to the IBS group. High-dose nanoparticles performed better than the marketed sustained-release capsule.

Conclusion

The chitosan–xanthan gum nanoparticle system enabled sustained, colon-specific delivery of mebeverine hydrochloride with superior therapeutic efficacy in vivo, offering a promising strategy for long-term IBS management.

Graphical abstract