Esomeprazole-Loaded Flash Release Sublingual Wafers: Formulation, Optimization, and Characterization

Purpose

The objective of the study was to develop sublingual wafers loaded with esomeprazole magnesium trihydrate (EMT) that exhibit rapid dissolution and enhanced penetration upon administration through sublingual mucosa, thereby ensuring immediate action.

Method

Sublingual wafers containing esomeprazole magnesium trihydrate were prepared using the solvent casting method. The formulation included different concentrations of hydroxypropyl methylcellulose E-15 (HPMC E-15), sodium starch glycolate (SSG), and polyethylene glycol 400 (PEG 400), as suggested by the DESIGN EXPERT software. An optimization strategy employing desirability values was utilized to optimize the responses. The wafers underwent physical characterization and in vitro dissolution study, followed by ex vivo drug permeation assessment and histopathological evaluation.

Results

The optimized sublingual wafers exhibited disintegration time of 27.67 ± 0.92 s, folding endurance of 299.71 ± 1.67, and drug content of 92.99 ± 3.37% with a percent deviation of less than 5. In vitro release study showed 82.92 ± 4.13% drug release in the 90s, following the Korsmeyer-Peppas mechanism. Ex vivo permeation demonstrated 80.07 ± 3.04% drug diffusion in 90 s. Histopathological investigations confirmed the safety of optimized wafers on sheep’s sublingual mucosa. Short-term stability study revealed the wafer’s stability for three months at 25–27 °C and 60% relative humidity.

Conclusion

The formulation of esomeprazole magnesium trihydrate (EMT)-loaded wafer is expected to enhance patient compliance by eliminating the requirement of water intake during the treatment of peptic ulcers and the need for swallowing. Moreover, the wafer offers a rapid onset of action and quick disintegration, providing a fast and convenient treatment option.