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

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Natural Product Chemistry

Background:

• Ferulic acid possesses antioxidant and anti-inflammatory properties but suffers from poor solubility.
• Gastric acid reflux and ulcers necessitate effective drug delivery systems for gastroprotection.

Purpose of the Study:

• To enhance ferulic acid solubility using solid dispersions.
• To formulate floating, mucoadhesive chewable tablets for controlled release and improved gastroprotection.
• To evaluate the antioxidant and anti-inflammatory potential of the developed ferulic acid formulation.

Main Methods:

• Solid dispersions of ferulic acid were prepared using Eudragit® E PO.
• Chewable tablets were formulated via direct compression with sodium alginate, calcium carbonate, HPMC, and mannitol.
• Tablets were evaluated for gel formation, buoyancy, acid neutralization capacity, drug release, and physical properties.
• In vitro antioxidant activity was assessed using the DPPH assay, and anti-inflammatory effects were studied in macrophage cells.

Main Results:

• The ferulic acid solid dispersion achieved a solubility of 39.9 mg/mL.
• Formulated tablets rapidly formed a gel layer, floated for over 8 hours, and exhibited sustained drug release (80.58% over 8 hours).
• The optimal formulation showed significant antioxidant activity (IC50 6.74 µg/mL) and superior anti-inflammatory effects compared to indomethacin.

Conclusions:

• Solid dispersion significantly enhanced ferulic acid solubility.
• The developed chewable tablets provide effective gastroprotection through acid neutralization, gel formation, and controlled release.
• This formulation holds promise for treating gastric ulcers and preventing acid reflux by enhancing ferulic acid's therapeutic efficacy.