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Background <p><i>Terminalia chebula</i> is widely used in Ayurvedic medicine, and chebulinic acid has been identified as a key bioactive constituent with notable antiulcer activity, owing to its antisecretory, antioxidant, and anti-inflammatory properties. However, chebulinic acid’s poor aqueous solubility and hydrophobic nature limit its pharmaceutical application.</p> Objectives <p>This study aimed to enhance the solubility, gastric retention, and therapeutic efficacy of chebulinic acid by developing chebulinic acid-loaded solid dispersions (CASD) incorporated into modified xanthan gum-coated sodium alginate-based gastroretentive beads for improved gastric ulcer treatment.</p> Methods <p>CASDs were prepared with PVP K30 <i>via</i> solvent evaporation and characterized using FTIR, XRD, and DSC. The optimized dispersion was incorporated into modified xanthan gum-coated sodium alginate gastroretentive floating beads through ionotropic gelation. Optimization was conducted using a Quality by Design approach with a Box–Behnken design. The resulting beads were evaluated for bead size, buoyancy, swelling, drug entrapment efficiency, surface morphology, in vitro drug release, and anti-ulcer activity to determine formulation performance.</p> Results <p>The optimized CASD demonstrated improved solubility (59.31&#xa0;mg/mL) and % cumulative drug release (93.03% within 2&#xa0;h) compared to pure chebulinic acid. Modified xanthan gum-coated sodium alginate beads achieved an encapsulation efficiency of 62.42%, a floating lag time of 6.1&#xa0;s, a density of 0.602&#xa0;g/cm³, a floating duration exceeding 24&#xa0;h, and sustained drug release of 74.8% over 8&#xa0;h. Quality by Design (QbD) optimization yielded a r² value greater than 0.9. In vivo studies showed 80.28% ulcer protection, comparable to that of omeprazole (82.04%).</p> Conclusions <p>CASD-loaded gastroretentive beads effectively enhanced the solubility, gastric retention, and antiulcer efficacy of chebulinic acid, highlighting their potential as an advanced delivery system for gastric ulcer management.</p> Graphical Abstract <p></p>

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QbD Enabled Chebulinic Acid Solid Dispersions Encapsulated in Modified Xanthan Gum Coated Sodium Alginate Beads for Enhanced Gastric Ulcer Therapy

  • 期刊论文

  • 发表日期：

    2026年4月24日

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  • Bigul Yogeshwar Bhardwaj,
  • Aditi Sharma,
  • Rohit Sharma,
  • Rohit Goyal,
  • Kaisar Raza,
  • Rakesh Pahwa,
  • Kamal Dua,
  • Sachin Kumar Singh,
  • Ram Prakash Dwivedi,
  • Jen Chang Yang,
  • Thakur Gurjeet Singh,
  • Poonam Negi

摘要

Background

Terminalia chebula is widely used in Ayurvedic medicine, and chebulinic acid has been identified as a key bioactive constituent with notable antiulcer activity, owing to its antisecretory, antioxidant, and anti-inflammatory properties. However, chebulinic acid’s poor aqueous solubility and hydrophobic nature limit its pharmaceutical application.

Objectives

This study aimed to enhance the solubility, gastric retention, and therapeutic efficacy of chebulinic acid by developing chebulinic acid-loaded solid dispersions (CASD) incorporated into modified xanthan gum-coated sodium alginate-based gastroretentive beads for improved gastric ulcer treatment.

Methods

CASDs were prepared with PVP K30 via solvent evaporation and characterized using FTIR, XRD, and DSC. The optimized dispersion was incorporated into modified xanthan gum-coated sodium alginate gastroretentive floating beads through ionotropic gelation. Optimization was conducted using a Quality by Design approach with a Box–Behnken design. The resulting beads were evaluated for bead size, buoyancy, swelling, drug entrapment efficiency, surface morphology, in vitro drug release, and anti-ulcer activity to determine formulation performance.

Results

The optimized CASD demonstrated improved solubility (59.31 mg/mL) and % cumulative drug release (93.03% within 2 h) compared to pure chebulinic acid. Modified xanthan gum-coated sodium alginate beads achieved an encapsulation efficiency of 62.42%, a floating lag time of 6.1 s, a density of 0.602 g/cm³, a floating duration exceeding 24 h, and sustained drug release of 74.8% over 8 h. Quality by Design (QbD) optimization yielded a r² value greater than 0.9. In vivo studies showed 80.28% ulcer protection, comparable to that of omeprazole (82.04%).

Conclusions

CASD-loaded gastroretentive beads effectively enhanced the solubility, gastric retention, and antiulcer efficacy of chebulinic acid, highlighting their potential as an advanced delivery system for gastric ulcer management.

Graphical Abstract