title: Preparation and Characterization of Microemulsions of Myricetin for Improving Its Antiproliferative and Antioxidative Activities and Oral Bioavailability.
abstract: To improve the bioactivity and oral bioavailability of myricetin, a microemulsion formulation was successfully developed, which consisted of Cremophor RH40 (12%), Tween 80 (6%), Transcutol HP (9%), WL 1349 (18%), and distilled water (55%). With lower content of surfactants and higher stability after dilution and storage for 6 months, the optimized myricetin microemulsion (MYR-ME) could dramatically enhance the solubility of myricetin 1225 times that in water. MYR-ME significantly increased antiproliferative activity against human cancer cell HepG2 without influence on normal cell LO2. It also notably improved the cellular antioxidative activity of myricetin. Furthermore, the oral bioavailability of myricetin was remarkably enhanced by MYR-ME in Sprague-Dawley rats after oral administration, which was 14.43-fold that with myricetin suspension. Therefore, the MYR-ME developed here could be used as a potential carrier for myricetin with substantially enhanced bioactivities and bioavailability and might promote myricetin's future utilization in functional foods and cosmetics.
authors.affiliation: School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, China.
authors.forename: Rui Xue
authors.initials: RX
authors.lastname: Guo
authors.affiliation: School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, China.
authors.forename: Xiong
authors.initials: X
authors.lastname: Fu
authors.affiliation: School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Chen
authors.affiliation: School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, China.|School of Biosciences and Biopharmaceutics, Guangdong Pharmaceutical University , Guangzhou 510006, China.
authors.forename: Lin
authors.initials: L
authors.lastname: Zhou
authors.affiliation: School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, China.
authors.forename: Gu
authors.initials: G
authors.lastname: Chen
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000737:chemistry* / Q000494:pharmacology*; D001682:Biological Availability; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000737:chemistry; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D006131:Growth Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D008297:Male; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D000975:Antioxidants; D004337:Drug Carriers; D004655:Emulsions; D005419:Flavonoids; D006131:Growth Inhibitors; D011136:Polysorbates; C040015:myricetin
keywords: antiproliferation; cellular antioxidative activity; microemulsion; myricetin; oral bioavailability