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Formulation and Characterization of Quercetin-loaded Oil in Water Nanoemulsion and Evaluation of Hypocholesterolemic Activity in Rats

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Department of Nutritional Science and Food Management, Ewha Womans University, Seoul 03760, Korea
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Department of Integrated Biomedical and Life Sciences, Korea University, Seoul 02841, Korea
3
Department of Food Science, University of Tennessee, Knoxville, TN 37996-6196, USA
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Kolmar BNH CO., LTd 2-15, Sandan-gil, Jeonui-myeon, Sejong-si 30003, Korea
5
R&D Center, EastHill Corporation, Gwonseon-gu, Suwon-si, Gyeonggi-do 16642, Korea
*
Authors to whom correspondence should be addressed.
Nutrients 2019, 11(2), 244; https://doi.org/10.3390/nu11020244
Received: 20 December 2018 / Revised: 16 January 2019 / Accepted: 17 January 2019 / Published: 22 January 2019
Due to poor water solubility and high susceptibility to chemical degradation, the applications of quercetin have been limited. This study investigated the effects of pH on the formation of quercetin-loaded nanoemulsion (NQ) and compared the hypocholesterolemic activity between quercetin and NQ to utilize the quercetin as functional food ingredient. NQ particle size exhibited a range of 207–289 nm with polydispersity index range (<0.47). The encapsulation efficiency increased stepwise from 56 to 92% as the pH increased from 4.0 to 9.0. Good stability of NQ was achieved in the pH range of 6.5–9.0 during 3-month storage at 21 and 37 °C. NQ displayed higher efficacy in reducing serum and hepatic cholesterol levels and increasing the release of bile acid into feces in rats fed high-cholesterol diet, compared to quercetin alone. NQ upregulated hepatic gene expression involved in bile acid synthesis and cholesterol efflux, such as cholesterol 7 alpha-hydroxylase (CYP7A1), liver X receptor alpha (LXRα), ATP-binding cassette transporter A1 (ABCA1) and ATP-binding cassette sub-family G member 1 (ABCG1). These results suggest at least partial involvement of hepatic bile acid synthesis and fecal cholesterol excretion in nanoemulsion quercetin-mediated beneficial effect on lipid abnormalities. View Full-Text
Keywords: quercetin; nanoemulsion; pH; stability; hypocholesterolemic activity quercetin; nanoemulsion; pH; stability; hypocholesterolemic activity
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Son, H.-Y.; Lee, M.-S.; Chang, E.; Kim, S.-Y.; Kang, B.; Ko, H.; Kim, I.-H.; Zhong, Q.; Jo, Y.-H.; Kim, C.-T.; Kim, Y. Formulation and Characterization of Quercetin-loaded Oil in Water Nanoemulsion and Evaluation of Hypocholesterolemic Activity in Rats. Nutrients 2019, 11, 244.

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