Abstract
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.
Highlights
Garcinia mangostana Linn., more commonly known as mangosteen (MG), belongs to the family Guttiferae [1,2]
Strong and steep peaks were seen as a result of intermolecular O–H stretching at wavenumbers (3458.47 and 3391.52 cm−1 ) in pure MGN spectrum and wavenumbers
MGN nanosponges were characterized by Fouriertransform infra-red (FTIR) spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), zeta potential, hydrodynamic diameter, entrapment efficiency, controlled drug release, and stability studies at stress conditions
Summary
Garcinia mangostana Linn., more commonly known as mangosteen (MG), belongs to the family Guttiferae [1,2]. The genus Garcinia is native to South-East Asian countries. The genus Garcinia is native to South‐East Asian countries com‐. Comprising more distinct species, each family reported distinct bioacprising more thanthan. 300 300 distinct species, withwith each family reported for for distinct bioactive tive compounds as xanthones, flavonoids, triterpenoids, benzophenones compounds suchsuch as xanthones, flavonoids, triterpenoids, and and benzophenones [3,4].[3,4]. The. The mangosteen pericarp possesses a therapeuticallyactive activecompound compound named mangostin mangosteen pericarp possesses a therapeutically mangostin (MGN) 1). The. Thetwo twoabundant abundant forms and γ) are present in pericarp the pericarp and (MGN) (Figure 1). Forms (α (α and γ) are present in the and xan‐. Xanthone constitutes structure of MGN [5,6]. Besides showing antihypertensive thone constitutes the the corecore structure of MGN
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