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.
Highlights
Diabetes mellitus (DM) is a major public health problem that represents, nowadays, an important concern due to its increasing prevalence and due to the challenges related to itstreatment, which isAppl
The size of CS–Gly microparticles was 822.00 ± 23.11 μm in wet state and 532.98 ± 40.08 μm in dry state, while the size of CS–lipoic acid (LA) microparticles was 1130.00 ± 31.25 μm in wet state and 916.73 ±
Despite the promising antidiabetic agents, the major challenges of diabetes mellitus treatment include optimizing the currently therapies in order to achieve an optimum and balanced glucose level, as well as reducing associated diabetes complications
Summary
Diabetes mellitus (DM) is a major public health problem that represents, nowadays, an important concern due to its increasing prevalence and due to the challenges related to itstreatment, which isAppl. Diabetes mellitus (DM) is a major public health problem that represents, nowadays, an important concern due to its increasing prevalence and due to the challenges related to itstreatment, which is. Sci. 2020, 10, 7532 one of the major causes of mortality [1]. The specific symptom of this chronic metabolic disorder is hyperglycemia due to a deficiency in insulin secretion, caused by damaged pancreatic beta-cells, or, peripherally, insulin resistance, or both of them [2]. The major target of antidiabetic therapy is to reduce the increased blood glucose level, which, in several cases, is very difficult to achieve [12]. Many antidiabetic drugs are responsible for different side effects, such as hypoglycemia, liver and kidney injury, weight gain, gastrointestinal disturbances, and hypersensitivity reactions [13,14]
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