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

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 treatme...

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Autores principales:	Faisal Usman, Hamid Saeed Shah, Sumera Zaib, Sirikhwan Manee, Jahanzeb Mudassir, Ajmal Khan, Gaber El-Saber Batiha, Khamael M. Abualnaja, Dalal Alhashmialameer, Imtiaz Khan
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	diabetes drug delivery α-glucosidase in vivo studies α-mangostin molecular docking Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/4bea49d723c44b938d3ac656fdc7cb5c
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spelling	oai:doaj.org-article:4bea49d723c44b938d3ac656fdc7cb5c2021-11-11T18:36:12ZFabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies10.3390/molecules262166331420-3049https://doaj.org/article/4bea49d723c44b938d3ac656fdc7cb5c2021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6633https://doaj.org/toc/1420-3049Type 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 α-mangostin (MGN), have been recognized to restore damaged pancreatic β-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 α-glucosidase and MGN in a protein-ligand complex. The maximum inhibition by nanosponges against α-glucosidase was observed to be 0.9352 ± 0.0856 µM, 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.Faisal UsmanHamid Saeed ShahSumera ZaibSirikhwan ManeeJahanzeb MudassirAjmal KhanGaber El-Saber BatihaKhamael M. AbualnajaDalal AlhashmialameerImtiaz KhanMDPI AGarticlediabetesdrug deliveryα-glucosidasein vivo studiesα-mangostinmolecular dockingOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6633, p 6633 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	diabetes drug delivery α-glucosidase in vivo studies α-mangostin molecular docking Organic chemistry QD241-441
spellingShingle	diabetes drug delivery α-glucosidase in vivo studies α-mangostin molecular docking Organic chemistry QD241-441 Faisal Usman Hamid Saeed Shah Sumera Zaib Sirikhwan Manee Jahanzeb Mudassir Ajmal Khan Gaber El-Saber Batiha Khamael M. Abualnaja Dalal Alhashmialameer Imtiaz Khan Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
description	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 α-mangostin (MGN), have been recognized to restore damaged pancreatic β-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 α-glucosidase and MGN in a protein-ligand complex. The maximum inhibition by nanosponges against α-glucosidase was observed to be 0.9352 ± 0.0856 µM, 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.
format	article
author	Faisal Usman Hamid Saeed Shah Sumera Zaib Sirikhwan Manee Jahanzeb Mudassir Ajmal Khan Gaber El-Saber Batiha Khamael M. Abualnaja Dalal Alhashmialameer Imtiaz Khan
author_facet	Faisal Usman Hamid Saeed Shah Sumera Zaib Sirikhwan Manee Jahanzeb Mudassir Ajmal Khan Gaber El-Saber Batiha Khamael M. Abualnaja Dalal Alhashmialameer Imtiaz Khan
author_sort	Faisal Usman
title	Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
title_short	Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
title_full	Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
title_fullStr	Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
title_full_unstemmed	Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies
title_sort	fabrication and biological assessment of antidiabetic α-mangostin loaded nanosponges: in vitro, in vivo, and in silico studies
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/4bea49d723c44b938d3ac656fdc7cb5c
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Fabrication and Biological Assessment of Antidiabetic α-Mangostin Loaded Nanosponges: In Vitro, In Vivo, and In Silico Studies

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