Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

Ther Deliv. 2022 Feb;13(2):81-93. doi: 10.4155/tde-2021-0062. Epub 2022 Jan 25.

Abstract

Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.

Keywords: Eudragit EPO; Terminalia chebula; antiulcer; chebulinic acid; raft system; solid dispersion.

MeSH terms

  • Hydrolyzable Tannins / pharmacology
  • Hydrolyzable Tannins / therapeutic use
  • Solubility
  • Stomach Ulcer* / chemically induced
  • Stomach Ulcer* / drug therapy
  • Terminalia*

Substances

  • Hydrolyzable Tannins
  • chebulinic acid