4.6 Article

Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies

期刊

MOLECULES
卷 26, 期 21, 页码 -

出版社

MDPI
DOI: 10.3390/molecules26216633

关键词

diabetes; drug delivery; alpha-glucosidase; in vivo studies; alpha-mangostin; molecular docking; nanosponges; quasi-emulsion method

资金

  1. Taif University, Saudi Arabia [TURSP-2020/267]

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Type 2 diabetes mellitus is a major health issue with increasing morbidity and mortality, and MGN-loaded nanosponges may be beneficial in the treatment of diabetes by prolonging the antidiabetic response in plasma and improving patient compliance via slow release of the drug and less frequent dosing.
Type 2 diabetes mellitus has been a major health issue with increasing morbidity and mortality due to macrovascular and microvascular complications. The urgent need for improved methods to control hyperglycemic complications reiterates the development of innovative preventive and therapeutic treatment strategies. In this perspective, xanthone compounds in the pericarp of the mangosteen fruit, especially alpha-mangostin (MGN), have been recognized to restore damaged pancreatic beta-cells for optimal insulin release. Therefore, taking advantage of the robust use of nanotechnology for targeted drug delivery, we herein report the preparation of MGN loaded nanosponges for anti-diabetic therapeutic applications. The nanosponges were prepared by quasi-emulsion solvent evaporation method. Physico-chemical characterization of formulated nanosponges with satisfactory outcomes was performed with Fourier transform infra-red (FTIR) spectroscopy, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Zeta potential, hydrodynamic diameter, entrapment efficiency, drug release properties, and stability studies at stress conditions were also tested. Molecular docking analysis revealed significant interactions of alpha-glucosidase and MGN in a protein-ligand complex. The maximum inhibition by nanosponges against alpha-glucosidase was observed to be 0.9352 & PLUSMN; 0.0856 mu M, 3.11-fold higher than acarbose. In vivo studies were conducted on diabetic rats and plasma glucose levels were estimated by HPLC. Collectively, our findings suggest that MGN-loaded nanosponges may be beneficial in the treatment of diabetes since they prolong the antidiabetic response in plasma and improve patient compliance by slowly releasing MGN and requiring less frequent doses, respectively.

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