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Purpose <p>The study aims to develop and assess colon-specific rifaximin (RFX) pellets for treating inflammatory bowel disease (IBD).</p> Method <p>Pellets were optimized for various coating ratios and coating levels of HPMC and Eudragit FS30D using Central Composite Design. Macroscopic evaluation and histopathological studies were performed to analyze their effects on colitic mucosa.</p> Result <p>Optimized formulation (R5) demonstrated the RFX release of 0.0%, 0.96 ± 0.03%, 33.06 ± 2.01%, and 90.03 ± 1.08% in 2&#xa0;h, 4&#xa0;h, 7&#xa0;h, and 12&#xa0;h, respectively. Gamma scintigraphy indicated that 99mTc-labeled RFX-pellets successfully targeted the colon in rabbits. The results showed no significant effect of radiolabeling on release characteristics from pellets. In R5 formulation, the average colon arrival timings, small intestine transit, and stomach emptying were evaluated and determined as 6.26 ± 0.142&#xa0;h, 5.72 ± 0.408&#xa0;h, and 0.70 ± 0.265&#xa0;h, respectively, in rabbits. RFX pellets- treated group exhibited a rise in colon length to approximately 10.1&#xa0;cm, indicating a return to baseline values which was significantly closer than in other colitis groups. The group treated with RFX pellets showed evidence of re-epithelization, and the histological characteristics corresponded to those of normal mice, thereby demonstrating a strong therapeutic impact on DSS-induced colitis.</p> Conclusion <p>Gamma scintigraphy and histological analyses verified colon targeting of RFX pellets and RFX efficacy in treating colitis related disorders.</p> Graphical Abstract

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Colon targeted rifaximin pellets: optimization, in vivo study, and gamma scintigraphy assessment

  • 期刊论文

  • 发表日期：

    2025年11月17日

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  • Ashwani Chaturvedi,
  • UVS Sara,
  • Ramdayal Gupta

摘要

Purpose

The study aims to develop and assess colon-specific rifaximin (RFX) pellets for treating inflammatory bowel disease (IBD).

Method

Pellets were optimized for various coating ratios and coating levels of HPMC and Eudragit FS30D using Central Composite Design. Macroscopic evaluation and histopathological studies were performed to analyze their effects on colitic mucosa.

Result

Optimized formulation (R5) demonstrated the RFX release of 0.0%, 0.96 ± 0.03%, 33.06 ± 2.01%, and 90.03 ± 1.08% in 2 h, 4 h, 7 h, and 12 h, respectively. Gamma scintigraphy indicated that 99mTc-labeled RFX-pellets successfully targeted the colon in rabbits. The results showed no significant effect of radiolabeling on release characteristics from pellets. In R5 formulation, the average colon arrival timings, small intestine transit, and stomach emptying were evaluated and determined as 6.26 ± 0.142 h, 5.72 ± 0.408 h, and 0.70 ± 0.265 h, respectively, in rabbits. RFX pellets- treated group exhibited a rise in colon length to approximately 10.1 cm, indicating a return to baseline values which was significantly closer than in other colitis groups. The group treated with RFX pellets showed evidence of re-epithelization, and the histological characteristics corresponded to those of normal mice, thereby demonstrating a strong therapeutic impact on DSS-induced colitis.

Conclusion

Gamma scintigraphy and histological analyses verified colon targeting of RFX pellets and RFX efficacy in treating colitis related disorders.

Graphical Abstract