Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies
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 we...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/4/491 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Waleed Y. Rizg |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-09T13:09:23Z |
| format | Article |
| id | doaj.art-24cbaf4cc1f54ef48116d97225efe6d8 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T13:09:23Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-24cbaf4cc1f54ef48116d97225efe6d82023-11-30T21:43:23ZengMDPI AGPharmaceuticals1424-82472022-04-0115449110.3390/ph15040491Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo StudiesWaleed Y. Rizg0N. Raghavendra Naveen1Mallesh Kurakula2Awaji Y. Safhi3Samar S. Murshid4Rayan Y. Mushtaq5Walaa A. Abualsunun6Majed Alharbi7Rana B. Bakhaidar8Alshaimaa M. Almehmady9Ahmad Salawi10Adel Al Fatease11Khaled M. Hosny12Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagar, Karnataka 571448, IndiaProduct Development Department, CURE Pharmaceutical, Oxnard, CA 93033, USADepartment of Pharmaceutics, Faculty of Pharmacy, Jazan University, Jazan 82817, Saudi ArabiaDepartment of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam 31441, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jazan University, Jazan 82817, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Khalid University, Abha 62529, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaSuccessful 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.https://www.mdpi.com/1424-8247/15/4/491sustainability of natural resourcesmicrospherethiolationmucoadhesionglibenclamidecentral composite design |
| spellingShingle | 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 Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies Pharmaceuticals sustainability of natural resources microsphere thiolation mucoadhesion glibenclamide central composite design |
| title | Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies |
| title_full | Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies |
| title_fullStr | Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies |
| title_full_unstemmed | Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies |
| title_short | Augmentation of Antidiabetic Activity of Glibenclamide Microspheres Using S-Protected Okra Powered by QbD: Scintigraphy and In Vivo Studies |
| title_sort | augmentation of antidiabetic activity of glibenclamide microspheres using s protected okra powered by qbd scintigraphy and in vivo studies |
| topic | sustainability of natural resources microsphere thiolation mucoadhesion glibenclamide central composite design |
| url | https://www.mdpi.com/1424-8247/15/4/491 |
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