Polymorphic Stability and Enhanced Drug Release of Dabigatran Etexilate Mesylate in Mesoporous Silica-Based Liquisolid Systems- Formulation and In Vitro Evaluation

Abstract

Purpose

Dabigatran etexilate mesylate, a BCS Class II drug used in the prevention of deep vein thrombosis and brain stroke, exhibits poor bioavailability and polymorphic tendencies. To address these challenges, this study focuses on formulating liquisolid compact tablets of dabigatran etexilate mesylate.

Methods

The liquisolid technique uses propylene glycol as a non-volatile solvent, with Neusilin US2 and microcrystalline cellulose (MCC) serving as carrier materials, and Syloid 244FP employed as a coating agent. The formulation was optimized through a central composite design to evaluate the effects of excipient ratio and super disintegrant concentration on flow properties and dissolution behavior.

Result

The optimized liquisolid formulation demonstrated enhanced solubility and drug release, with 91.07% cumulative drug release compared to directly compressible tablets. Differential scanning calorimetry (DSC) measurements and powder X-ray diffraction (PXRD) analyses confirmed the molecular dispersion of the drug and the preservation of its crystalline Form III. Stability studies indicated no significant changes in dissolution profiles or physical properties over three months.

Conclusion

This study demonstrates the effectiveness of the liquisolid technique in enhancing the solubility, dissolution rate, and stability of dabigatran etexilate mesylate while also preventing polymorphic transformation.