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Formulation and Characterization of Quercetin-loaded Oil in Water Nanoemulsion and Evaluation of Hypocholesterolemic Activity in Rats
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 ut...
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Published in: | Nutrients 2019-01, Vol.11 (2), p.244 |
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description | 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 ( |
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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.</description><identifier>ISSN: 2072-6643</identifier><identifier>EISSN: 2072-6643</identifier><identifier>DOI: 10.3390/nu11020244</identifier><identifier>PMID: 30678282</identifier><language>eng</language><publisher>Switzerland: MDPI AG</publisher><subject>ABC transporters ; Animals ; Antioxidants - chemistry ; Antioxidants - pharmacology ; Bile ; Bile acids ; Bioavailability ; Biopolymers ; blood serum ; Cardiovascular disease ; chemical degradation ; cholesteremic effect ; Cholesterol ; Cholesterol, Dietary - administration & dosage ; Cocoa ; Curcumin ; Emulsions - chemistry ; encapsulation ; enzymes ; excretion ; Fat metabolism ; feces ; Food ; Fruits ; functional foods ; Garlic ; gene expression ; gene expression regulation ; Green tea ; Hesperidin ; High density lipoprotein ; high fat diet ; Homeostasis ; Hypercholesterolemia - drug therapy ; ingredients ; Intestine ; Lipid metabolism ; Lipids ; liver ; Low density lipoprotein ; Male ; Metabolism ; Nanoemulsions ; Nanostructures ; Natural resources ; Oil ; oils ; Particle size ; Polyphenols ; Quercetin ; Quercetin - chemistry ; Quercetin - therapeutic use ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Sodium ; Surface tension ; Surfactants ; Tea ; Vegetable oils ; water solubility</subject><ispartof>Nutrients, 2019-01, Vol.11 (2), p.244</ispartof><rights>2019. This work is licensed under https://creativecommons.org/licenses/by/4.0/ (the “License”). 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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.</description><subject>ABC transporters</subject><subject>Animals</subject><subject>Antioxidants - chemistry</subject><subject>Antioxidants - pharmacology</subject><subject>Bile</subject><subject>Bile acids</subject><subject>Bioavailability</subject><subject>Biopolymers</subject><subject>blood serum</subject><subject>Cardiovascular disease</subject><subject>chemical degradation</subject><subject>cholesteremic effect</subject><subject>Cholesterol</subject><subject>Cholesterol, Dietary - administration & dosage</subject><subject>Cocoa</subject><subject>Curcumin</subject><subject>Emulsions - chemistry</subject><subject>encapsulation</subject><subject>enzymes</subject><subject>excretion</subject><subject>Fat metabolism</subject><subject>feces</subject><subject>Food</subject><subject>Fruits</subject><subject>functional foods</subject><subject>Garlic</subject><subject>gene expression</subject><subject>gene expression regulation</subject><subject>Green tea</subject><subject>Hesperidin</subject><subject>High density lipoprotein</subject><subject>high fat diet</subject><subject>Homeostasis</subject><subject>Hypercholesterolemia - 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Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Nutrients</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Son, Hye-Yeon</au><au>Lee, Mak-Soon</au><au>Chang, Eugene</au><au>Kim, Seog-Young</au><au>Kang, Bori</au><au>Ko, Hyunmi</au><au>Kim, In-Hwan</au><au>Zhong, Qixin</au><au>Jo, Young-Hee</au><au>Kim, Chong-Tai</au><au>Kim, Yangha</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation and Characterization of Quercetin-loaded Oil in Water Nanoemulsion and Evaluation of Hypocholesterolemic Activity in Rats</atitle><jtitle>Nutrients</jtitle><addtitle>Nutrients</addtitle><date>2019-01-22</date><risdate>2019</risdate><volume>11</volume><issue>2</issue><spage>244</spage><pages>244-</pages><issn>2072-6643</issn><eissn>2072-6643</eissn><abstract>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.</abstract><cop>Switzerland</cop><pub>MDPI AG</pub><pmid>30678282</pmid><doi>10.3390/nu11020244</doi><orcidid>https://orcid.org/0000-0002-7280-7597</orcidid><orcidid>https://orcid.org/0000-0001-6266-5460</orcidid><orcidid>https://orcid.org/0000-0001-6949-7666</orcidid><oa>free_for_read</oa></addata></record> |
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subjects | ABC transporters Animals Antioxidants - chemistry Antioxidants - pharmacology Bile Bile acids Bioavailability Biopolymers blood serum Cardiovascular disease chemical degradation cholesteremic effect Cholesterol Cholesterol, Dietary - administration & dosage Cocoa Curcumin Emulsions - chemistry encapsulation enzymes excretion Fat metabolism feces Food Fruits functional foods Garlic gene expression gene expression regulation Green tea Hesperidin High density lipoprotein high fat diet Homeostasis Hypercholesterolemia - drug therapy ingredients Intestine Lipid metabolism Lipids liver Low density lipoprotein Male Metabolism Nanoemulsions Nanostructures Natural resources Oil oils Particle size Polyphenols Quercetin Quercetin - chemistry Quercetin - therapeutic use Random Allocation Rats Rats, Sprague-Dawley Sodium Surface tension Surfactants Tea Vegetable oils water solubility |
title | Formulation and Characterization of Quercetin-loaded Oil in Water Nanoemulsion and Evaluation of Hypocholesterolemic Activity in Rats |
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