CLC number: R945
On-line Access: 2019-03-01
Received: 2018-06-22
Revision Accepted: 2018-10-14
Crosschecked: 2019-01-10
Cited: 0
Clicked: 6748
Su-fang Gu, Li-ying Wang, Ying-jie Tian, Zhu-xian Zhou, Jian-bin Tang, Xiang-rui Liu, Hai-ping Jiang, You-qing Shen. Enhanced water solubility, antioxidant activity, and oral absorption of hesperetin by
@article{title="Enhanced water solubility, antioxidant activity, and oral absorption of hesperetin by
author="Su-fang Gu, Li-ying Wang, Ying-jie Tian, Zhu-xian Zhou, Jian-bin Tang, Xiang-rui Liu, Hai-ping Jiang, You-qing Shen",
journal="Journal of Zhejiang University Science B",
volume="20",
number="3",
pages="273-281",
year="2019",
publisher="Zhejiang University Press & Springer",
doi="10.1631/jzus.B1800346"
}
%0 Journal Article
%T Enhanced water solubility, antioxidant activity, and oral absorption of hesperetin by
%A Su-fang Gu
%A Li-ying Wang
%A Ying-jie Tian
%A Zhu-xian Zhou
%A Jian-bin Tang
%A Xiang-rui Liu
%A Hai-ping Jiang
%A You-qing Shen
%J Journal of Zhejiang University SCIENCE B
%V 20
%N 3
%P 273-281
%@ 1673-1581
%D 2019
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.B1800346
TY - JOUR
T1 - Enhanced water solubility, antioxidant activity, and oral absorption of hesperetin by
A1 - Su-fang Gu
A1 - Li-ying Wang
A1 - Ying-jie Tian
A1 - Zhu-xian Zhou
A1 - Jian-bin Tang
A1 - Xiang-rui Liu
A1 - Hai-ping Jiang
A1 - You-qing Shen
J0 - Journal of Zhejiang University Science B
VL - 20
IS - 3
SP - 273
EP - 281
%@ 1673-1581
Y1 - 2019
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.B1800346
Abstract: hesperetin, an abundant bioactive component of citrus fruits, is poorly water-soluble, resulting in low oral bioavailability. We developed new formulations to improve the water solubility, antioxidant activity, and oral absorption of hesperetin. Two nano-based formulations were developed, namely hesperetin-TPGS (
[1]Attili-Qadri S, Karra N, Nemirovski A, et al., 2013. Oral delivery system prolongs blood circulation of docetaxel nanocapsules via lymphatic absorption. Proc Natl Acad Sci USA, 110(43):17498-17503.
[2]Brand W, van der Wel PAI, Rein MJ, et al., 2008. Metabolism and transport of the citrus flavonoid hesperetin in Caco-2 cell monolayers. Drug Metab Dispos, 36(9):1794-1802.
[3]Choudhury H, Gorain B, Pandey M, et al., 2017. Recent advances in TPGS-based nanoparticles of docetaxel for improved chemotherapy. Int J Pharm, 529(1-2):506-522.
[4]de Souza VT, de Franco ÉPD, de Araújo MEMB, et al., 2016. Characterization of the antioxidant activity of aglycone and glycosylated derivatives of hesperetin: an in vitro and in vivo study. J Mol Recognit, 29(2):80-87.
[5]Dintaman JM, Silverman JA, 1999. Inhibition of P-glycoprotein by
[6]Kanaze FI, Bounartzi MI, Georgarakis M, et al., 2007. Pharmacokinetics of the citrus flavanone aglycones hesperetin and naringenin after single oral administration in human subjects. Eur J Clin Nutr, 61(4):472-477.
[7]Khan J, Alexander A, Ajazuddin, et al., 2013. Recent advances and future prospects of phyto-phospholipid complexation technique for improving pharmacokinetic profile of plant actives. J Control Release, 168(1):50-60.
[8]Kim HJ, Jeon SM, Lee MK, et al., 2010. Comparison of hesperetin and its metabolites for cholesterol-lowering and antioxidative efficacy in hypercholesterolemic hamsters. J Med Food, 13(4):808-814.
[9]Krasavage WJ, Terhaar CJ, 1977. d-α-Tocopheryl poly(ethylene glycol) 1000 succinate. Acute toxicity, subchronic feeding, reproduction, and teratologic studies in the rat. J Agric Food Chem, 25(2):273-278.
[10]Li Y, Yang DJ, Chen SL, et al., 2008. Process parameters and morphology in puerarin, phospholipids and their complex microparticles generation by supercritical antisolvent precipitation. Int J Pharm, 359(1-2):35-45.
[11]Liu LX, Chen J, 2008. Solubility of hesperetin in various solvents from (288.2 to 323.2) K. J Chem Eng Data, 53(7):1649-1650.
[12]Maiti K, Mukherjee K, Murugan V, et al., 2009. Exploring the effect of hesperetin-HSPC complex—a novel drug delivery system on the in vitro release, therapeutic efficacy and pharmacokinetics. AAPS PharmSciTech, 10(3):943-950.
[13]Németh K, Plumb GW, Berrin JG, et al., 2003. Deglycosylation by small intestinal epithelial cell β-glucosidases is a critical step in the absorption and metabolism of dietary flavonoid glycosides in humans. Eur J Nutr, 42(1):29-42.
[14]Parhiz H, Roohbakhsh A, Soltani F, et al., 2015. Antioxidant and anti-inflammatory properties of the citrus flavonoids hesperidin and hesperetin: an updated review of their molecular mechanisms and experimental models. Phytother Res, 29(3):323-331.
[15]Qin LH, Niu YW, Wang YM, et al., 2018. Combination of phospholipid complex and submicron emulsion techniques for improving oral bioavailability and therapeutic efficacy of water-insoluble drug. Mol Pharm, 15(3):1238-1247.
[16]Roohbakhsh A, Parhiz H, Soltani F, et al., 2014. Neuropharmacological properties and pharmacokinetics of the citrus flavonoids hesperidin and hesperetin—a mini-review. Life Sci, 113(1-2):1-6.
[17]Shete G, Pawar YB, Thanki K, et al., 2015. Oral bioavailability and pharmacodynamic activity of hesperetin nanocrystals generated using a novel bottom-up technology. Mol Pharm, 12(4):1158-1170.
[18]Shin GH, Li JL, Cho JH, et al., 2016. Enhancement of curcumin solubility by phase change from crystalline to amorphous in cur-TPGS nanosuspension. J Food Sci, 81(2):N494-N501.
[19]Singh H, Narang JK, Singla YP, et al., 2017. TPGS stabilized sublingual films of frovatriptan for the management of menstrual migraine: formulation, design and antioxidant activity. J Drug Deliv Sci Technol, 41:144-156.
[20]Testai L, Calderone V, 2017. Nutraceutical value of citrus flavanones and their implications in cardiovascular disease. Nutrients, 9(5):502.
[21]Varma MVS, Panchagnula R, 2005. Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo. Eur J Pharm Sci, 25(4-5):445-453.
[22]Wang JN, Wang LL, Zhang L, et al., 2018. Studies on the curcumin phospholipid complex solidified with Soluplus®. J Pharm Pharmacol, 70(2):242-249.
[23]Wolfe KL, Liu RH, 2007. Cellular antioxidant activity (CAA) assay for assessing antioxidants, foods, and dietary supplements. J Agric Food Chem, 55(22):8896-8907.
[24]Zhang ZP, Tan SW, Feng SS, 2012. Vitamin E TPGS as a molecular biomaterial for drug delivery. Biomaterials, 33(19):4889-4906.
[25]Zhao BX, Gu SF, Du Y, et al., 2018. Solid lipid nanoparticles as carriers for oral delivery of hydroxysafflor yellow A. Int J Pharm, 535(1-2):164-171.
Open peer comments: Debate/Discuss/Question/Opinion
<1>