A comprehensive development strategy in buccal drug delivery.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Buccal drug delivery offers an alternative route for systemic administration, bypassing first-pass metabolism.
• Developing effective mucoadhesive formulations requires optimizing drug-polymer interactions and release kinetics.
• Omeprazole, a model drug, presents challenges in buccal delivery due to its physicochemical properties.

Purpose of the Study:

• To develop and characterize an integrated mucoadhesive matrix for buccal administration of omeprazole.
• To investigate the influence of cyclodextrin complexation and alkali agents on mucoadhesion, drug release, and permeation.
• To identify an optimal formulation balancing mucoadhesion, dissolution, and permeation properties.

Main Methods:

• Formulation of mucoadhesive tablets with omeprazole (free or complexed with cyclodextrins) and alkali agents.
• Evaluation of mucoadhesion using factorial analysis.
• In vitro drug release studies employing model-dependent and independent analyses.
• Permeation studies using porcine buccal mucosa.
• Analysis of drug release kinetics using the Korsmeyer-Peppas model.

Main Results:

• Drug hydrophobicity negatively impacted mucoadhesion; cyclodextrin complexation improved it, with methyl-β-cyclodextrin showing superior results.
• L-arginine, an alkali agent, also influenced mucoadhesion and release profiles.
• The optimal drug release profile was achieved with omeprazole complexed with methyl-β-cyclodextrin in the presence of L-arginine.
• Drug release followed super case II transport kinetics, indicating a diffusion-erosion mechanism.
• Maximum drug permeation was observed with the methyl-β-cyclodextrin complexed formulation containing L-arginine.

Conclusions:

• The developed mucoadhesive matrix, incorporating methyl-β-cyclodextrin complexed omeprazole and L-arginine, demonstrates significant potential for buccal drug delivery.
• This formulation achieves a favorable balance of mucoadhesion, dissolution, and permeation characteristics.
• The integrated strategy provides a robust approach for optimizing buccal drug delivery systems.