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<p>Famotidine, a lipophilic H<sub>2</sub>-antagonist, suffers from limited oral bioavailability (40–45%) due to poor aqueous solubility. This study aimed to enhance its solubility and therapeutic potential via a nanoemulsion (NE) system prepared by spontaneous emulsification. Pseudoternary phase diagrams guided the selection of olive oil, Tween 80, and PEG 400 (Smix 3:1 and 4:1 ratios) as formulation components. The optimized NE formulation (F2) exhibited a droplet size of 13.25&#xa0;nm, low polydispersity index (0.100), and high transmittance (98.61%). In vitro release studies showed F2 achieved 80.32% drug release within 180&#xa0;min compared to 51.61% for the pure drug. Permeability studies demonstrated higher intestinal absorption for F2 (0.27 per mL) than pure drug (0.20 per mL) at 180&#xa0;min. In vivo antiulcer studies using an aspirin-induced ulcer model in rats revealed an ulcer inhibition of 88.65% for F2 versus 45% for standard famotidine suspension. Stability testing confirmed consistent clarity and drug content over 60&#xa0;days under refrigerated and ambient conditions. These findings confirm that the developed nanoemulsion significantly improves famotidine’s solubility, absorption, and antiulcer efficacy, offering a promising strategy for enhancing the oral bioavailability of poorly water-soluble drugs.</p> Graphical Abstract <p></p>

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Design and Evaluation of Nanoemulsified Famotidine for Enhanced Permeability and Antiulcer Potential

  • 期刊论文

  • 发表日期：

    2025年9月27日

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  • Atit Pandey,
  • Sonam M. Gandhi,
  • Naitikkumar D. Trivedi,
  • Gajendra S. Rathore,
  • Devesh U. Kapoor

摘要

Famotidine, a lipophilic H2-antagonist, suffers from limited oral bioavailability (40–45%) due to poor aqueous solubility. This study aimed to enhance its solubility and therapeutic potential via a nanoemulsion (NE) system prepared by spontaneous emulsification. Pseudoternary phase diagrams guided the selection of olive oil, Tween 80, and PEG 400 (Smix 3:1 and 4:1 ratios) as formulation components. The optimized NE formulation (F2) exhibited a droplet size of 13.25 nm, low polydispersity index (0.100), and high transmittance (98.61%). In vitro release studies showed F2 achieved 80.32% drug release within 180 min compared to 51.61% for the pure drug. Permeability studies demonstrated higher intestinal absorption for F2 (0.27 per mL) than pure drug (0.20 per mL) at 180 min. In vivo antiulcer studies using an aspirin-induced ulcer model in rats revealed an ulcer inhibition of 88.65% for F2 versus 45% for standard famotidine suspension. Stability testing confirmed consistent clarity and drug content over 60 days under refrigerated and ambient conditions. These findings confirm that the developed nanoemulsion significantly improves famotidine’s solubility, absorption, and antiulcer efficacy, offering a promising strategy for enhancing the oral bioavailability of poorly water-soluble drugs.

Graphical Abstract