Publication: Oral empagliflozin-loaded tri-layer core-sheath fibers fabricated using tri-axial electrospinning: Enhanced in vitro and in vivo antidiabetic performance
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Date
2023-03-25
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Abstract
Empagliflozin (EM) was successfully loaded in polycaprolactone/poly (L-lactic acid)/polymethyl methacrylate (PCL/PLA/PMMA) fibers. In the rat β-cell line (BRIN-BD11), the insulin expression ratio of pancreatic β-cells was stimulated at high and low glucose by culturing with tri-layer EM-loaded fiber (EMF) for 48 h. The expression ratios of glucokinase and GLUT-2 proteins increased after EMF treatment. According to the in vitro drug release test, 97% of all drug contained in fibers was released in a controlled manner for 24 h. The pharmacokinetic test revealed that the bioavailability was improved ∼4.8-fold with EMF treatment compared to EM-powder and blood glucose level was effectively controlled for 24 h with EMF. Oral administration of EMF exhibited a better sustainable anti-diabetic activity even in the half-dosage than EM-powder in streptozotocin/nicotinamide-induced T2DM rats. The levels of GLP-1, PPAR-γ, and insulin were increased while the levels of SGLT-2 and TNF-α were decreased with EMF treatment. Also, EMF recovered the histopathological changes in the liver, pancreas, and kidney in T2DM rats and protected pancreatic β-cells. Consequently, EMF is suggested as an unprecedented and promotive treatment approach for T2DM with a higher bioavailability and better antidiabetic effect compared to conventional dosage forms.
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Tıp, Sağlık Bilimleri, Medicine, Health Sciences, Klinik Tıp (MED), Klinik Tıp, TROPİKAL TIP, Clinical Medicine (MED), CLINICAL MEDICINE, TROPICAL MEDICINE, Farmasötik bilim, Yaşam Bilimleri, Pharmaceutical Science, Life Sciences, Core-sheath fiber, Empagliflozin, Insulin resistance, Tri-axial electrospinning, Type 2 diabetes mellitus
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Guler E., Nur Hazar-Yavuz A., TATAR E., Morid Haidari M., Sinemcan Ozcan G., DURUKSU G., Graça M. P. F., Kalaskar D. M., GÜNDÜZ O., Emin Cam M., "Oral empagliflozin-loaded tri-layer core-sheath fibers fabricated using tri-axial electrospinning: Enhanced in vitro and in vivo antidiabetic performance", International Journal of Pharmaceutics, cilt.635, 2023