Abstract
Probucol (PB) is a highly lipophilic drug with potential protective effects on pancreatic β-cells from inflammation and oxidation. PB has poor bioavailability and solubility, and despite many attempts, significant improvement in antidiabetic effects or absorption has yet to be discovered. Recently, the role of bile acids has been established in significant drug formulation stabilisation effects and as cell-penetrating agents. Promising results in pharmaceutical formulation studies on drug stability and release patterns when lithocholic acid (LCA) is conjugated with PB and sodium alginate (SA) have been demonstrated. Thus, this study aimed to develop and characterise PB microcapsules incorporating LCA and examine the biological effects of the microcapsules in vitro and in vivo. PB/LCA microcapsules were prepared using an encapsulation method, ionic gelation vibrational jet flow technology. LCA incorporation in PB microcapsules showed positive effects on β-cells with improved insulin release, antioxidant activity, and PB intracellular uptake. Diabetic mice gavaged LCA-PB microcapsules showed a significant reduction in diabetes signs and symptoms, better survival rate, reduced blood glucose levels, and pro-inflammatory cytokines, with an increase PB level in blood and tissues suggesting a potential therapy for treating diabetes mellitus.
Highlights
Diabetes mellitus (DM) is a metabolic disorder characterised by high blood glucose and inflammation and is categorised as type 1 (T1D) or type 2 (T2D) [1]
The results showed no significant difference in body weight, 10 water of 18 intake, survival rate, blood glucose, and pro-inflammatory cytokines expression between mice gavaged with PB-loaded G-3 and PB-lithocholic acid (LCA)-loaded G-4 microcapsules
The results showed no significant difference in body weight, water intake, survival rate, blood glucose, and pro-inflammatory cytokines expression between mice gavaged with PB-loaded G-3 and PB-LCA-loaded G-4 microcapsules
Summary
Diabetes mellitus (DM) is a metabolic disorder characterised by high blood glucose and inflammation and is categorised as type 1 (T1D) or type 2 (T2D) [1]. It is one of the most significant health challenges of this decade and has an enormous burden on economic and health systems globally [2,3]. Reports indicate that almost one in three pre-diabetic patients will develop T2D if no effective interventions, such as early diagnosis, diet, and lifestyle changes, are employed [6,7].
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