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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Tsinghua University Press
2023-11-01
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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 |
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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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institution | Kabale University |
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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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