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Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies

Authors :
Waleed Y. Rizg
N. Raghavendra Naveen
Mallesh Kurakula
Awaji Y. Safhi
Samar S. Murshid
Rayan Y. Mushtaq
Walaa A. Abualsunun
Majed Alharbi
Rana B. Bakhaidar
Alshaimaa M. Almehmady
Ahmad Salawi
Adel Al Fatease
Khaled M. Hosny
Source :
Pharmaceuticals, Vol 15, Iss 4, p 491 (2022)
Publication Year :
2022
Publisher :
MDPI AG, 2022.

Abstract

Successful drug delivery by mucoadhesive systems depends on the polymer type, which usually gets adherent on hydration. The intended polymers must sustain the association with biomembranes and preserve or accommodate the drug for an extended time. The majority of hydrophilic polymers tend to make weak interactions like noncovalent bonds, which hampers the positioning of dosage forms at the required target sites, leading to inefficient therapeutic outcomes. It is possible to overcome this by functionalizing the natural polymers with thiol moiety. Further, considering that S-protected thiomers can benefit by improving thiol stability at a broad range of pH and enhancing the residence period at the required target, 2-mercapto-nicotinic acid (MA) was utilized in this present study to shield the free thiol groups on thiolated okra (TO). S-protected TO (STO) was synthesized and characterized for various parameters. Glibenclamide-loaded microspheres were formulated using STO (G-STO-M), and the process was optimized. The optimized formulation has shown complete and controlled release of the loaded drug at the end of the dissolution study. Cell viability assay indicated that the thiolated S-protected polymers gelated very well, and the formulated microspheres were safe. Further, G-STO-M showed considerable in vivo mucoadhesion strength. The glucose tolerance test confirmed the efficacy of STO formulation in minimizing the plasma glucose level. These results favor S-protection as an encouraging tool for improving the absorption of poorly aqueous soluble drugs like glibenclamide.

Details

Language :
English
ISSN :
14248247
Volume :
15
Issue :
4
Database :
Directory of Open Access Journals
Journal :
Pharmaceuticals
Publication Type :
Academic Journal
Accession number :
edsdoj.24cbaf4cc1f54ef48116d97225efe6d8
Document Type :
article
Full Text :
https://doi.org/10.3390/ph15040491