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Food Science and Human Wellness 2023, 12(6): 2306-2313 https://doi.org/10.1016/j.fshw.2023.03.034
Research Article | Open Access | Issue | Published: 04 April 2023

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

Show Author's Information Ying Lia,  Hang Sua,  Wenjun Wanga,  Zhongping Yina,  Jing'en Lia,  En Yuanb,  Qingfeng Zhanga( )
Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China

Peer review under responsibility of KeAi Communications Co., Ltd.

Keywords:
Characterization, Bioavailability, Taxifolin, Zein nanoparticles
Cite this article:
Li Y, Su H, Wang W, et al. Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rat. Food Science and Human Wellness, 2023, 12(6): 2306-2313. https://doi.org/10.1016/j.fshw.2023.03.034
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Abstract Full text About this article

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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About this article

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

Show Author's information Ying Lia, Hang Sua, Wenjun Wanga, Zhongping Yina, Jing'en Lia, En Yuanb, Qingfeng Zhanga( )
Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China

Peer review under responsibility of KeAi Communications Co., Ltd.

Abstract

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.

Keywords: Characterization, Bioavailability, Taxifolin, Zein nanoparticles

References(38)

[1]

S. Zu, L. Yang, J. Huang, et al., Micronization of taxifolin by supercritical antisolvent process and evaluation of radical scavenging activity, Int. J. Mol. Sci. 13 (2012) 8869-8881. http://doi.org/10.3390/ijms13078869.
DOI Google Scholar
[2]

B. Abad-García, S. Garmón-Lobato, L.A. Berrueta, et al., A fragmentation study of dihydroquercetin using triple quadrupole mass spectrometry and its application for identification of dihydroflavonols in Citrus juices, Rapid Commun. Mass Spectrom. 23 (2019) 2785-2792. http://doi.org/10.1002/rcm.4182.
DOI Google Scholar
[3]

D. Turck, J. Bresson, B. Burlingame, et al., Scientific opinion on taxifolin-rich extract from Dahurian Larch (Larix gmelinii), EFSA J. 15 (2017) e04682. http://doi.org/10.2903/j.efsa.2017.4682.
DOI Google Scholar
[4]

C. Sunil, B. Xu, An insight into the health-promoting effects of taxifolin (dihydroquercetin), Phytochemistry 166 (2019) 112066. http://doi.org/10.1016/j.phytochem.2019.112066.
DOI Google Scholar
[5]

A.E. Weidmann, Dihydroquercetin: More than just an impurity? Eur. J. Pharmacol. 684 (2012) 19-26. http://doi.org/10.1016/j.ejphar.2012.03.035.
DOI Google Scholar
[6]

A. Das, R. Baidya, T. Chakraborty, et al., Pharmacological basis and new insights of taxifolin: a comprehensive review, Biomed. Pharmacother. 142 (2021) 112004. https://doi.org/10.1016/j.biopha.2021.112004.
DOI Google Scholar
[7]

F.C. Stenger Moura, N. Pinna, R. Vivani, et al., Exploring taxifolin polymorphs: insights on hydrate and anhydrous forms, Pharmaceutics 13 (2021) 1328. https://doi.org/10.3390/pharmaceutics13091328.
DOI Google Scholar
[8]

X.D. Wang, M.X. Meng, L.B. Gao, et al., Permeation of astilbin and taxifolin in Caco-2 cell and their effects on the P-gp, Int. J. Pharm. 378 (2009) 1-8. http://doi.org/10.1016/j.ijpharm.2009.05.022.
DOI Google Scholar
[9]

X. Wang, H. Xia, F. Xing, et al., A highly sensitive and robust UPLC-MS with electrospray ionization method for quantitation of taxifolin in rat plasma, J. Chromatogr. B. 877 (2009) 1778-1786. http://doi.org/10.1016/j.jchromb.2009.04.037.
DOI Google Scholar
[10]

C.J. Yang, Z.B. Wang, Y.Y. Mi, et al., UHPLC-MS/MS determination, pharmacokinetic, and bioavailability study of taxifolin in rat plasma after oral administration of its nanodispersion, Molecules 21 (2016) 494. http://doi.org/10.3390/molecules21040494.
DOI Google Scholar
[11]

O.N. Pozharitskaya, M.V. Karlina, A.N. Shikov, et al., Determination and pharmacokinetic study of taxifolin in rabbit plasma by high-performance liquid chromatography, Phytomedicine 16 (2009) 244-251. http://doi.org/10.1016/j.phymed.2008.10.002.
DOI Google Scholar
[12]

A.N. Shikov, O.N. Pozharitskaya, I. Miroshnyk, et al., Nanodispersions of taxifolin: impact of solid-state properties on dissolution behavior, Int. J. Pharm. 377 (2009) 148-152. http://doi.org/10.1016/j.ijpharm.2009.04.044.
DOI Google Scholar
[13]

M.V. Karlina, O.N. Pozharitskaya, A.N. Shikov, Development and in vitro biopharmaceutical evaluation of a dihydroquercetin microemulsion. Pharm. Chem. J. 43 (2009) 352. https://doi.org/10.1007/s11094-009-0308-x.
DOI Google Scholar
[14]

F. Hasibi, A. Nasirpour, J. Varshosaz, et al., Formulation and characterization of taxifolin-loaded lipid nanovesicles (liposomes, niosomes, and transfersomes) for beverage fortification, Eur. J. Lipid Sci. Technol. 122 (2020) 1900105. https://doi.org/10.1002/ejlt.201900105.
DOI Google Scholar
[15]

J.M. Irache, C.J. González-Navarro, Zein nanoparticles as vehicles for oral delivery purposes, Nanomedicine 12 (2017) 1209-1211. 10.2217/nnm-2017-0075.
DOI Google Scholar
[16]

Y. Luo, Q. Wang, Zein-based micro-and nano-particles for drug and nutrient delivery: a review, J. Appl. Polym. Sci. 131 (2014) 1107-1117. http://doi.org/10.1002/app.40696.
DOI Google Scholar
[17]

T. Zou, L. Gu, TPGS emulsified zein nanoparticles enhanced oral bioavailability of daidzin: in vitro characteristics and in vivo performance, Mol. Pharmaceutics 10 (2013) 2062-2070. http://doi.org/10.1021/mp400086n.
DOI Google Scholar
[18]

D. Zheng, Q.F. Zhang, Bioavailability enhancement of astilbin in rats through zein-caseinate nanoparticles, J. Agric. Food Chem. 67 (2019) 5746-5753. http://doi.org/10.1021/acs.jafc.9b00018.
DOI Google Scholar
[19]

C.C. Sun, H. Su, G.D. Zheng, et al., Fabrication and characterization of dihydromyricetin encapsulated zein-caseinate nanoparticles and its bioavailability in rat, Food Chem. 330 (2020) 127245. http://doi.org/10.1016/j.foodchem.2020.127245.
DOI Google Scholar
[20]

X.L. Qiu, Q.F. Zhang, Acidic hydrolysis of astilbin and its application for the preparation of taxifolin from Rhizoma Smilacis Glabrae, J. Chem. Res. 45 (2021) 290-294. http://doi.org/10.1177/1747519820948357.
DOI Google Scholar
[21]

United States Pharmacopeia, Simulated gastric fluid and simulated intestinal fluid, TS. The United States Pharmacopeia, 23, The National Formularly (1995) 2207-2235.
Google Scholar
[22]

Q.F. Zhang, Y.J. Fu, Z.W. Huang, et al., Aqueous stability of astilbin: effects of pH, temperature, and solvent, J. Agric. Food Chem. 61 (2013) 12085-12091. http://doi.org/10.1021/jf404420s.
DOI Google Scholar
[23]

D. Zheng, C.C. Sun, H. Su, et al., Metabolism, excretion, and tissue distribution of astilbin-zein nanoparticles in rats, J. Agric. Food Chem. 67 (2019) 8332-8338. http://doi.org/10.1021/acs.jafc.9b02569.
DOI Google Scholar
[24]

A.R. Patel, E.C. Bouwens, K.P. Velikov, Sodium caseinate stabilized zein colloidal particles, J. Agric. Food Chem. 58 (2010) 12497-12503. http://doi.org/10.1021/jf102959b.
DOI Google Scholar
[25]

C. Chang, T. Wang, Q. Hu, et al., Caseinate-zein-polysaccharide complex nanoparticles as potential oral delivery vehicles for curcumin: effect of polysaccharide type and chemical cross-linking, Food Hydrocoll. 72 (2017) 254-262. http://doi.org/10.1016/j.foodhyd.2017.05.039.
DOI Google Scholar
[26]

L. Dai, C. Sun, R. Li, et al., Structural characterization, formation mechanism and stability of curcumin in zein-lecithin composite nanoparticles fabricated by antisolvent co-precipitation, Food Chem. 237 (2017) 1163-1171. https://doi.org/10.1016/j.foodchem.2017.05.134.
DOI Google Scholar
[27]

A.R. Patel, P.C. Heussen, J. Hazekamp, et al., Quercetin loaded biopolymeric colloidal particles prepared by simultaneous precipitation of quercetin with hydrophobic protein in aqueous medium, Food Chem. 133 (2012) 423-429. https://doi.org/10.1016/j.foodchem.2012.01.054.
DOI Google Scholar
[28]

Z. Li, H. Jiang, C. Xu, et al., A review: using nanoparticles to enhance absorption and bioavailability of phenolic phytochemicals, Food Hydrocoll. 43 (2015) 153-164. http://doi.org/10.1016/j.foodhyd.2014.05.010.
DOI Google Scholar
[29]

G. Williamson, C.D. Kay, A. Crozier, The bioavailability, transport, and bioactivity of dietary flavonoids: a review from a historical perspective, Compr. Rev. Food Sci. F. 17 (2018) 1054-1112. http://doi.org/10.1111/1541-4337.12351.
DOI Google Scholar
[30]

S.H. Thilakarathna, H.P. Rupasinghe, Flavonoid bioavailability and attempts for bioavailability enhancement, Nutrients 5 (2013) 3367-3387. http://doi.org/10.3390/nu5093367.
DOI Google Scholar
[31]

P. Yang, F. Xu, H.F. Li, et al., Detection of 191 taxifolin metabolites and their distribution in rats using HPLC-ESI-IT-TOF-MSn, Molecules 21 (2016) 1209. http://doi.org/10.3390/molecules21091209.
DOI Google Scholar
[32]

B. Ge, L. Zhao, X. Li, et al., Glucuronidation is the dominating in vivo metabolism pathway of herbacetin: elucidation of herbacetin pharmacokinetics after intravenous and oral administration in rats, J. Funct. Foods 40 (2018) 659-669. http://doi.org/10.1016/j.jff.2017.12.006.
DOI Google Scholar
[33]

A. Crozier, I.B. Jaganath, M.N. Clifford, Dietary phenolics: chemistry, bioavailability and effects on health, Nat. Prod. Rep. 26 (2009) 1001-1043. http://doi.org/10.1039/b802662a.
DOI Google Scholar
[34]

X.J. Tian, X.W. Yang, X. Yang, et al., Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model. Int. J. Pharm. 367 (2009) 58-64. http://doi.org/10.1016/j.ijpharm.2008.09.023.
DOI Google Scholar
[35]

M. Hu, Commentary: bioavailability of flavonoids and polyphenols: call to arms, Mol. Pharmaceutics 4 (2007) 803-806. http://doi.org/10.1021/mp7001363.
DOI Google Scholar
[36]

J.M. Landete, Updated knowledge about polyphenols: functions, bioavailability, metabolism, and health, Rev. Food Sci. Nutr. 52 (2012) 936-948. http://doi.org/10.1080/10408398.2010.513779.
DOI Google Scholar
[37]

A.M. Nectoux, C. Abe, S.W. Huang, et al., Absorption and metabolic behavior of hesperidin (Rutinosylated Hesperetin) after single oral administration to sprague-dawley rats, J. Agric. Food Chem. 67 (2019) 9812-9819. http://doi.org/10.1021/acs.jafc.9b03594.
DOI Google Scholar
[38]

A.J. Day, F. Mellon, D. Barron, et al., Human metabolism of dietary flavonoids: identification of plasma metabolites of quercetin, Free Radical Res. 35 (2001) 941-952. http://doi.org/10.1080/10715760100301441.
DOI Google Scholar
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Publication history

Received: 16 September 2021
Revised: 30 October 2021
Accepted: 29 November 2021
Published: 04 April 2023
Issue date: November 2023

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© 2023 Beijing Academy of Food Sciences.

Acknowledgements

This work was supported by the National Natural Science Foundation of China (32060541).

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This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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