Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat

Taxifolin loaded zein-caseinate nanoparticles (TZP) were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat. The formulations of TZP were optimized. With mass ratio of 1:1:2 between taxifolin, zein and sodium caseinate, the par...

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Main Authors: Ying Li, Hang Su, Wenjun Wang, Zhongping Yin, Jing’en Li, En Yuan, Qingfeng Zhang
Format: Article
Language:English
Published: Tsinghua University Press 2023-11-01
Series:Food Science and Human Wellness
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Online Access:http://www.sciencedirect.com/science/article/pii/S2213453023000861
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author Ying Li
Hang Su
Wenjun Wang
Zhongping Yin
Jing’en Li
En Yuan
Qingfeng Zhang
author_facet Ying Li
Hang Su
Wenjun Wang
Zhongping Yin
Jing’en Li
En Yuan
Qingfeng Zhang
author_sort Ying Li
collection DOAJ
description Taxifolin loaded zein-caseinate nanoparticles (TZP) were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat. The formulations of TZP were optimized. With mass ratio of 1:1:2 between taxifolin, zein and sodium caseinate, the particle size and ζ-potential of TZP were (168.74 ± 0.35) nm and (−57.67 ± 0.25) mV, while the encapsulation and loading efficiency of taxifolin were (85.83 ± 0.89)% and (17.11 ± 0.88)%, respectively. After freeze-drying, TZP exhibited excellent redispersibility in water without aggregation. Physicochemical characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was observed. After encapsulating in TZP, the excellent dispersion of taxifolin in water significantly improve its diffusion velocity through a semi-permeable membrane. After oral administration, taxifolin and its five metabolites were identified in rat plasma by ultra high performance liquid chromatography (UPLC) with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The dynamic variation of taxifolin and its metabolites in plasma were then quantified by UPLC with a triple-quadrupole typemass spectroscopy (UPLC-QqQ-MS/MS). A pharmacokinetic study showed that the bioavailability of taxifolin increased from 0.35 % to 0.52 % through TZP fabrication. The plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than taxifolin. Glucuronidation was the dominating metabolism pathway of taxifolin in vivo.
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spelling doaj-art-5e80ff9ee8b24bbb87734bbf8005fca32025-02-03T05:55:57ZengTsinghua University PressFood Science and Human Wellness2213-45302023-11-0112623062313Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in ratYing Li0Hang Su1Wenjun Wang2Zhongping Yin3Jing’en Li4En Yuan5Qingfeng Zhang6Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, ChinaJiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, ChinaJiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, ChinaJiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, ChinaJiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, ChinaCollege of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, ChinaJiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China; Corresponding author at: Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China.Taxifolin loaded zein-caseinate nanoparticles (TZP) were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat. The formulations of TZP were optimized. With mass ratio of 1:1:2 between taxifolin, zein and sodium caseinate, the particle size and ζ-potential of TZP were (168.74 ± 0.35) nm and (−57.67 ± 0.25) mV, while the encapsulation and loading efficiency of taxifolin were (85.83 ± 0.89)% and (17.11 ± 0.88)%, respectively. After freeze-drying, TZP exhibited excellent redispersibility in water without aggregation. Physicochemical characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was observed. After encapsulating in TZP, the excellent dispersion of taxifolin in water significantly improve its diffusion velocity through a semi-permeable membrane. After oral administration, taxifolin and its five metabolites were identified in rat plasma by ultra high performance liquid chromatography (UPLC) with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The dynamic variation of taxifolin and its metabolites in plasma were then quantified by UPLC with a triple-quadrupole typemass spectroscopy (UPLC-QqQ-MS/MS). A pharmacokinetic study showed that the bioavailability of taxifolin increased from 0.35 % to 0.52 % through TZP fabrication. The plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than taxifolin. Glucuronidation was the dominating metabolism pathway of taxifolin in vivo.http://www.sciencedirect.com/science/article/pii/S2213453023000861TaxifolinZein nanoparticlesCharacterizationBioavailability
spellingShingle Ying Li
Hang Su
Wenjun Wang
Zhongping Yin
Jing’en Li
En Yuan
Qingfeng Zhang
Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
Food Science and Human Wellness
Taxifolin
Zein nanoparticles
Characterization
Bioavailability
title Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
title_full Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
title_fullStr Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
title_full_unstemmed Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
title_short Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat
title_sort fabrication of taxifolin loaded zein caseinate nanoparticles and its bioavailability in rat
topic Taxifolin
Zein nanoparticles
Characterization
Bioavailability
url http://www.sciencedirect.com/science/article/pii/S2213453023000861
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