Engineered gastroretentive amorphous ferulate matrix: a novel raft-forming paradigm for enhanced bioavailability.

Abstract

This study aimed to enhance the solubility of ferulic acid using solid dispersion techniques and develop chewable tablets that neutralize stomach acid, form a protective gel layer, prevent gastric fluid reflux, and ensure prolonged retention in the stomach with controlled release of the active ingredient. Researchers developed solid dispersions of ferulic acid using Eudragit^® E PO as a carrier, with a 1:2 w/w ratio, achieving the highest solubility (39.9 mg/mL). Chewable tablets were formulated by direct compression, incorporating sodium alginate as a gelling agent, calcium carbonate for calcium ions and carbon dioxide, HPMC as a release retardant, and mannitol as a diluent. All formulations rapidly formed a gel layer within 10 s, had a lower density than gastric fluid, and floated on 0.1 N hydrochloric acid for over 8 h. The optimal formulation demonstrated excellent physical properties, including a gel strength of 11.84 g, an acid neutralization capacity of 15.97 mEq, and reaching 80.58% over 8 h with gradual release. It exhibited significant antioxidant activity (IC₅₀ 6.74 µg/mL) in the DPPH assay and showed stronger anti-inflammatory effects in macrophage cells than indomethacin. These findings suggest this formulation could enhance ferulic acid's effectiveness in treating gastric ulcers and preventing acid reflux.