Design and Optimization of Quercetin-Loaded Polymeric Eudragit L-100 Nanoparticles for Anti-diabetic Activity with Improved Oral Delivery: In-Vitro and In-Vivo Evaluation
Abstract To design and develop a nanoformulation from isolated quercetin (QT) from the Annona reticulata Linn leaves to enhance therapeutic index, solubility, bioavailability, toxicity mitigation, pharmacological activity improvement, and prevention of physical and chemical degradation of antidiabetic lead compounds. Bio-flavonoids are gaining popularity in diabetes and other therapeutic research due to their various pharmacological and biological effects. QT is one of several beneficial flavonoids, has amazing hypoglycemic effects, with significant improvement, stabilization of long-term insulin secretion, and regeneration of human islets in the pancreas without causing severe health risks. However, poor solubility, biological milieu instability, limited permeation, short biological half-life, and low bioavailability prevent its widespread use in anti-diabetic research. This novel approach of polymeric nanoformulation of QT will improve the bioavailability and enhance its antidiabetic activity. The effectiveness of QT-loaded Eudragit L-100 (EDL) nanoparticles (NPs) against hyperglycemia in streptozotocin-induced type 2 diabetic rats was investigated in this work. QT/EDLNPs were designed by Box–Behnken Design and prepared by a sonication-assisted emulsification solvent evaporation process. The optimized QT/EDLNPs formulation was administered orally for 21 days to streptozotocin-induced diabetic rats. The QT/EDLNPs demonstrated significant antidiabetic effects comparable to the currently available anti-diabetic drug Glibenclamide. Thus, the approach provides an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. These findings suggest that QT/EDLNPs is an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. This study also investigates a fantastic alternative method for creating brand-new polymeric NPs that serve as bioactive compound delivery systems.Journal instruction requires a city for affiliations; however, these are missing in affiliation 2. Please verify if the provided city is correct and amend if necessary.City for affiliation 2 is Dibrugarh.It is correctPlease confirm if the author names are presented accurately and in the correct sequence (given name, middle name/initial, family name). Author Given name: [Mohammad Zaki], Last name [Ahmad], Given name: [Ratna Jyoti], Last name [Das].The author names are presented accurately.It is confirmed.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:33 |
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| Enthalten in: |
Journal of inorganic and organometallic polymers and materials - 33(2023), 8 vom: 11. Mai, Seite 2411-2428 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ahmad, Mohammad Zaki [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
Antidiabetic activity |
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| Anmerkungen: |
© The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. |
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| doi: |
10.1007/s10904-023-02694-w |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Abstract To design and develop a nanoformulation from isolated quercetin (QT) from the Annona reticulata Linn leaves to enhance therapeutic index, solubility, bioavailability, toxicity mitigation, pharmacological activity improvement, and prevention of physical and chemical degradation of antidiabetic lead compounds. Bio-flavonoids are gaining popularity in diabetes and other therapeutic research due to their various pharmacological and biological effects. QT is one of several beneficial flavonoids, has amazing hypoglycemic effects, with significant improvement, stabilization of long-term insulin secretion, and regeneration of human islets in the pancreas without causing severe health risks. However, poor solubility, biological milieu instability, limited permeation, short biological half-life, and low bioavailability prevent its widespread use in anti-diabetic research. This novel approach of polymeric nanoformulation of QT will improve the bioavailability and enhance its antidiabetic activity. The effectiveness of QT-loaded Eudragit L-100 (EDL) nanoparticles (NPs) against hyperglycemia in streptozotocin-induced type 2 diabetic rats was investigated in this work. QT/EDLNPs were designed by Box–Behnken Design and prepared by a sonication-assisted emulsification solvent evaporation process. The optimized QT/EDLNPs formulation was administered orally for 21 days to streptozotocin-induced diabetic rats. The QT/EDLNPs demonstrated significant antidiabetic effects comparable to the currently available anti-diabetic drug Glibenclamide. Thus, the approach provides an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. These findings suggest that QT/EDLNPs is an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. This study also investigates a fantastic alternative method for creating brand-new polymeric NPs that serve as bioactive compound delivery systems.Journal instruction requires a city for affiliations; however, these are missing in affiliation 2. Please verify if the provided city is correct and amend if necessary.City for affiliation 2 is Dibrugarh.It is correctPlease confirm if the author names are presented accurately and in the correct sequence (given name, middle name/initial, family name). Author Given name: [Mohammad Zaki], Last name [Ahmad], Given name: [Ratna Jyoti], Last name [Das].The author names are presented accurately.It is confirmed | ||
| 650 | 4 | |a Polymeric nanoparticles |7 (dpeaa)DE-He213 | |
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| 650 | 4 | |a Eudragit |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Experimental design |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Box–Behnken |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Optimization |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Antidiabetic activity |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Pathak, Kalyani |4 aut | |
| 700 | 1 | |a Das, Ratna Jyoti |4 aut | |
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| 700 | 1 | |a Gogoi, Neelutpal |4 aut | |
| 700 | 1 | |a Gogoi, Urvashee |4 aut | |
| 700 | 1 | |a Das, Aparoop |4 aut | |
| 700 | 1 | |a Alasiri, Ali S. |4 aut | |
| 700 | 1 | |a Abdel-Wahab, Basel A. |4 aut | |
| 700 | 1 | |a Abdullah, M. M. |4 aut | |
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