o:34045 Liposome Encapsulation Enhances the Antidiabetic Efficacy of Silibinin en ABSTRACT Silibinin has considerable therapeutic potential for the treatment of diabetes through anti-inflammatory, antioxidant, and immunomodulatory properties. However, the therapeutic application of silibinin is quite limited due to its poor bioavailability. In the present study, an attempt was made to improve the antidiabetic efficacy of silibinin by its encapsulation in liposomal vesicles. The liposomes with a high encapsulation efficiency of silibinin (96%) and a zeta potential of −26.2 ± 0.6 mV were developed and studied using nicotinamide/streptozotocin-induced diabetic rats. Administration of silibinin-loaded liposomes to diabetic rats lowered glucose levels, increased insulin levels, and improved pancreatic islet architecture. The anti-inflammatory effect of silibinin-loaded liposomes was demonstrated by a decrease in serum C-reactive protein (CRP) levels and a reduced deposition of collagen fibers in the islets of diabetic rats. Furthermore, silibinin-loaded liposomes were more efficient in lowering glucose, alanine transaminase, triglyceride, and creatinine levels in diabetic rats than pure silibinin. In addition, silibinin-loaded liposomes had a significantly better effect on beta-cell mass and Glut2 glucose receptor distribution in diabetic islets than pure silibinin. The present results clearly show that liposome encapsulation of silibinin enhances its antidiabetic efficacy, which may contribute to the therapeutic benefit of silibinin in the treatment of diabetes and its complications. diabetes; insulin; silibinin; liposomes; antidiabetic; anti-inflammatory; C-reactive protein; collagen deposition 1552099 10.3390/pharmaceutics16060801 2024-06-18T08:55:03.285Z 44 yes 46 Svetlana Dinić Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia Jelena Arambašić Jovanović Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Aleksandra Uskoković Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Aleksandra Jovanović University of Belgrade, Institute for the Application of Nuclear Energy INEP, Serbia doktor tehnoloških nauka person 0000-0001-5394-0125 Nevena Grdović Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Jovana Rajić Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Marija Đorđević Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Ana Sarić Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Branko Bugarski Faculty of Technology and Metallurgy, University of Belgrade, Serbia person Melita Vidaković Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person Mirjana Mihailović Department of Molecular Biology, Institute for Biological Research “Siniša Stanković”-National Institute of the Republic of Serbia, University of Belgrade, Serbia person application/pdf 4104120 https://phaidrabg.bg.ac.rs/o:34045 no yes 16 70 92000001 11A21 11A2102 11A29 11A2910 11A41 Pharmaceutics 16 6 MDPI 2024