title: Encapsulation and Delivery of Crystalline Hydrophobic Nutraceuticals using Nanoemulsions: Factors Affecting Polymethoxyflavone Solubility.
abstract: Polymethoxyflavones (PMF) isolated from citrus peel have potent anti-cancer activity, however their utilization as functional ingredients in foods is currently limited because of their high melting point and poor water-solubility. The influence of oil type and concentration, hydrophilic polymer addition, and simulated intestinal conditions on PMF (5-hydroxytangeretin) solubility in solutions and nanoemulsions was examined. The saturation concentration of PMF in water was relatively low (0.93 µM), but could be increased appreciably by adding certain hydrophilic polymers: polyethylene glycol (PEG) and β-cyclodextrin (CD) were ineffective at increasing solubility, but poly(vinyl alcohol) (PVA) and hydroxypropyl methylcellulose (HPMC) greatly enhanced solubility (e.g., > 6 µM for 0.5 % polymer). PMF was more soluble in medium chain triglycerides (MCT, 6.1 mM) than long chain triglycerides (LCT, 4.2 mM). The encapsulation efficiency of PMF in oil-in-water nanoemulsions was higher when MCT was used as the oil phase rather than LCT, and could be increased by increasing the oil droplet content. The solubility of PMF in simulated small intestinal fluids was increased by solubilization in bile micelles and mixed micelles formed during lipid digestion. These results have important implications for the development of functional foods fortified with bioactive hydrophobic components aimed at improving human health and wellness.
authors: Biopolymers and Colloids Research Laboratory, Department of Food Science, University of Massachusetts, Amherst, MA 01003, USA.
authors: Yan
authors: Y
authors: Li
authors: Hang
authors: H
authors: Xiao
authors: David Julian
authors: DJ
authors: McClements
keywords: Bioavailability; Flavonoids; Nanoemulsions; Nanoparticles; Nutraceuticals; Pharmaceuticals
references: J Biotechnol. 2004 Sep 30;113(1-3):151-70
references: 15380654
references: Adv Drug Deliv Rev. 2008 Mar 17;60(6):615-6
references: 18160174
references: Adv Colloid Interface Sci. 2012 Jun 15;174:1-30
references: 22475330
references: Int J Pharm. 2011 Nov 25;420(1):1-10
references: 21884771
references: Expert Opin Drug Deliv. 2012 Jun;9(6):687-700
references: 22519507
references: Mol Pharm. 2011 Apr 4;8(2):564-70
references: 21268663
references: Eur J Pharm Biopharm. 2011 May;78(1):125-33
references: 21168491
references: Int J Pharm. 2011 Sep 15;416(1):55-60
references: 21679756
references: Life Sci. 2001 Jul 13;69(8):901-13
references: 11488403
references: J Nutr. 2007 Oct;137(10):2229-33
references: 17885003
references: J Chromatogr A. 2010 Jan 29;1217(5):642-7
references: 20022018
references: Int J Pharm. 2003 Jan 2;250(1):3-11
references: 12480268
references: Adv Drug Deliv Rev. 2001 Oct 1;50 Suppl 1:S127-47
references: 11576699
references: Mol Pharm. 2012 May 7;9(5):1100-8
references: 22376012
references: J Pharm Sci. 2010 Nov;99(11):4525-34
references: 20845451
references: Comb Chem High Throughput Screen. 2011 Jun 1;14(5):328-38
references: 21470182
references: Food Hydrocoll. 2012 Jun 1;27(2):517-528
references: 22685367
references: J Pharm Sci. 2003 Dec;92(12):2386-98
references: 14603484
references: Carcinogenesis. 2008 Dec;29(12):2415-24
references: 18820286
references: J Pharm Pharmacol. 2010 Nov;62(11):1656-68
references: 21039549
references: Chemphyschem. 2006 Dec 11;7(12):2601-6
references: 17109452
references: Annu Rev Food Sci Technol. 2010;1:241-69
references: 22129337
references: Adv Drug Deliv Rev. 2007 Jul 30;59(7):645-66
references: 17601630
references: Pharm Res. 2006 Sep;23(9):2165-74
references: 16902814
references: J Pharm Sci. 2010 Dec;99(12):4982-91
references: 20574997
references: Life Sci. 2006 Dec 23;80(3):245-53
references: 17046027
references: J Pharm Sci. 2009 Aug;98(8):2549-72
references: 19373886
references: Int J Pharm. 2012 Jul 1;430(1-2):388-91
references: 22465550
references: J Drug Target. 2010 Dec;18(10):704-31
references: 20973755
references: Nat Rev Drug Discov. 2007 Mar;6(3):231-48
references: 17330072
references: Mol Nutr Food Res. 2007 Dec;51(12):1478-84
references: 17979096
references: Food Funct. 2012 Mar;3(3):202-20
references: 22105669
references: Food Chem. 2012 Sep 15;134(2):1106-12
references: 23107734
references: Bioorg Med Chem. 2009 Jan 1;17(1):25-8
references: 19054677
references: Mol Pharm. 2011 Oct 3;8(5):1910-8
references: 21875119
references: J Agric Food Chem. 2006 Jun 14;54(12):4176-85
references: 16756344
references: Mol Nutr Food Res. 2009 Mar;53(3):398-406
references: 19065586
references: J Agric Food Chem. 2007 Oct 31;55(22):8950-7
references: 17927194
references: Carcinogenesis. 2007 Dec;28(12):2581-8
references: 17962218
references: Crit Rev Food Sci Nutr. 2011 Apr;51(4):285-330
references: 21432697
references: J Pharm Sci. 2002 Aug;91(8):1743-64
references: 12115803
references: Adv Drug Deliv Rev. 2007 Jul 30;59(7):667-76
references: 17618704