Chitosan-Based Delivery Systems Loaded with Glibenclamide and Lipoic Acid: Formulation, Characterization, and Kinetic Release Studies

Abstract

Glibenclamide and lipoic acid are two drugs frequently recommended for the management of diabetes mellitus, and so, the development of a new formulation containing both substances has a great benefit in terms of efficiency and compliance, acting also as a multi-target drug system. Accordingly, the aim of this study was the formulation and physicochemicalcharacterization of new polymeric systems based on chitosan (CS) in whose matrix were encapsulated glibenclamide (Gly) and lipoic acid (LA). The polymeric systems were prepared as microparticles (CS–Gly, CS–LA, and CS–Gly–LA) through ionic gelation method, using pentasodium tripolyphosphate (TPP) as crosslinking agent. The polymeric systems obtained were characterized in terms of particle size and morphology, IR spectroscopy, entrapment efficiency and drug loading, swelling degree, and therelease of the active substances from the chitosan matrix. The polymeric systems obtained were stable systems; the presence of glibenclamide and lipoic acid into the polymer matrix were proved by IR spectroscopy. The entrapment efficiency was 94.66% for Gly and 39.68% for LA. The developed polymeric systems proved a favorable swelling degree and drug release profile, the percentage of release being 88.68% for LA and 75.17% for Gly from CS–Gly–LA systems.

Keywords

• chitosan
• glibenclamide
• lipoic acid
• drug delivery systems