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Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin

Quercetin (QR) is a naturally occurring flavonoid organic compound that has poor solubility in water and highly unstable in alkaline conditions, resulting in limited absorption in poultry. Consequently, in our experiment, QR was employed as a model compound, encapsulated within the caffeic acid graf...

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Autores principales: Ren, Xin, Ren, Juan, Li, Yipeng, Yuan, Sikun, Wang, Gengnan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10354432/
https://www.ncbi.nlm.nih.gov/pubmed/37476826
http://dx.doi.org/10.3389/fvets.2023.1218025
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author Ren, Xin
Ren, Juan
Li, Yipeng
Yuan, Sikun
Wang, Gengnan
author_facet Ren, Xin
Ren, Juan
Li, Yipeng
Yuan, Sikun
Wang, Gengnan
author_sort Ren, Xin
collection PubMed
description Quercetin (QR) is a naturally occurring flavonoid organic compound that has poor solubility in water and highly unstable in alkaline conditions, resulting in limited absorption in poultry. Consequently, in our experiment, QR was employed as a model compound, encapsulated within the caffeic acid graft chitosan copolymer (CA-g-CS) self-assembled micelles to enhance its solubility, stability and exhibit a synergistic antibacterial effect. The optimization of the formula was carried out using a combination of single-factor experimentation and the response surface method. The in vitro release rate and stability of CA-g-CS-loaded QR micelles (CA-g-CS/QR) in various pH media were studied and the pharmacokinetics in white feather broiler chickens was evaluated in vivo. Additionally, the antibacterial activity was investigated using Escherichia coliCMCC44102 and Escherichia coli of chicken origin as the test strain. The results showed the optimized formula for the self-assembled micelles were 4 mL water, 0.02 mg/mL graft copolymer, and 1 mg QR, stirring at room temperature. The encapsulation efficiency was 72.09%. The resulting CA-g-CS/QR was uniform in size with an average diameter of 375.6 ± 5.9 nm. The release pattern was consistent with the Ritger-Peppas model. CA-g-CS/QR also significantly improved the stability of QR in alkaline condition. The relative bioavailability of CA-g-CS/QR was found to be 1.67-fold that of the reference drug, indicating a substantial increase in the absorption of QR in the broiler. Compared to the original drug, the antibacterial activity of CA-g-CS/QR was significantly enhanced, as evidenced by a reduction of half in the MIC and MBC values. These results suggest that CA-g-CS/QR improves the bioavailability and antibacterial activity of QR, making it a promising candidate for clinical use.
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spelling pubmed-103544322023-07-20 Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin Ren, Xin Ren, Juan Li, Yipeng Yuan, Sikun Wang, Gengnan Front Vet Sci Veterinary Science Quercetin (QR) is a naturally occurring flavonoid organic compound that has poor solubility in water and highly unstable in alkaline conditions, resulting in limited absorption in poultry. Consequently, in our experiment, QR was employed as a model compound, encapsulated within the caffeic acid graft chitosan copolymer (CA-g-CS) self-assembled micelles to enhance its solubility, stability and exhibit a synergistic antibacterial effect. The optimization of the formula was carried out using a combination of single-factor experimentation and the response surface method. The in vitro release rate and stability of CA-g-CS-loaded QR micelles (CA-g-CS/QR) in various pH media were studied and the pharmacokinetics in white feather broiler chickens was evaluated in vivo. Additionally, the antibacterial activity was investigated using Escherichia coliCMCC44102 and Escherichia coli of chicken origin as the test strain. The results showed the optimized formula for the self-assembled micelles were 4 mL water, 0.02 mg/mL graft copolymer, and 1 mg QR, stirring at room temperature. The encapsulation efficiency was 72.09%. The resulting CA-g-CS/QR was uniform in size with an average diameter of 375.6 ± 5.9 nm. The release pattern was consistent with the Ritger-Peppas model. CA-g-CS/QR also significantly improved the stability of QR in alkaline condition. The relative bioavailability of CA-g-CS/QR was found to be 1.67-fold that of the reference drug, indicating a substantial increase in the absorption of QR in the broiler. Compared to the original drug, the antibacterial activity of CA-g-CS/QR was significantly enhanced, as evidenced by a reduction of half in the MIC and MBC values. These results suggest that CA-g-CS/QR improves the bioavailability and antibacterial activity of QR, making it a promising candidate for clinical use. Frontiers Media S.A. 2023-07-05 /pmc/articles/PMC10354432/ /pubmed/37476826 http://dx.doi.org/10.3389/fvets.2023.1218025 Text en Copyright © 2023 Ren, Ren, Li, Yuan and Wang. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Veterinary Science
Ren, Xin
Ren, Juan
Li, Yipeng
Yuan, Sikun
Wang, Gengnan
Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title_full Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title_fullStr Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title_full_unstemmed Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title_short Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
title_sort preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
topic Veterinary Science
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10354432/
https://www.ncbi.nlm.nih.gov/pubmed/37476826
http://dx.doi.org/10.3389/fvets.2023.1218025
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