Sublingual Administration of Teucrium Polium-Loaded Nanofibers with Ultra-Fast Release in the Treatment of Diabetes Mellitus: In Vitro and In Vivo Evaluation.

J Pharm Sci

Department of Pharmacology, Faculty of Pharmacy, Marmara University, Istanbul 34854, Turkiye; Department of Pharmacology, Faculty of Pharmacy, Istanbul Kent University, Istanbul 34406, Türkiye; Center for Nanotechnology and Biomaterials Application and Research, Marmara University, Istanbul 34722, Turkiye; MecNano Technologies, Cube Incibation, Teknopark Istanbul, Istanbul 34906, Türkiye; Genetic and Metabolic Diseases Research and Investigation Center, Marmara University, Istanbul 34722, Turkiye; Biomedical Engineering Department, University of Aveiro, Aveiro 3810-193, Portugal; SFA R&D Laboratories, Teknopark Istanbul, Istanbul 34906, Türkiye; ATA BIO Technology, Teknopol Istanbul, Istanbul 34930, Türkiye. Electronic address:

Published: April 2024

In this study, Teucrium polium (TP) methanolic extract, which has antidiabetic activity and protects the β-cells of the pancreas, was loaded in polyethylene oxide/sodium alginate nanofibers by electrospinning and administered sublingually to evaluate their effectiveness in type-2 diabetes mellitus (T2DM) by cell culture and in vivo studies. The gene expressions of insulin, glucokinase, GLUT-1, and GLUT-2 improved in TP-loaded nanofibers (TPF) on human beta cells 1.1B4 and rat beta cells BRIN-BD11. Fast-dissolving (<120 s) sublingual TPF exhibited better sustainable anti-diabetic activity than the suspension form, even in the twenty times lower dosage in streptozotocin/nicotinamide-induced T2DM rats. The levels of GLP-1, GLUT-2, SGLT-2, PPAR-γ, insulin, and tumor necrosis factor-alpha were improved. TP and TPF treatments ameliorated morphological changes in the liver, pancreas, and kidney. The fiber diameter increased, tensile strength decreased, and the working temperature range enlarged by loading TP in fibers. Thus, TPF has proven to be a novel supportive treatment approach for T2DM with the features of being non-toxic, easy to use, and effective.

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http://dx.doi.org/10.1016/j.xphs.2023.12.013DOI Listing

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