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Encapsulation and Delivery of Crystalline Hydrophobic Nutraceuticals using Nanoemulsions: Factors Affecting Polymethoxyflavone Solubility

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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.

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Acknowledgments

This work was supported in part by an EPA-NSF-NIFA (AFRI) joint grant (2010-05266) program, NIH grant CA139174, a USDA-AFRI grant, a special call grant from Massachusetts Center for Agriculture, and a CVIP grant from the University of Massachusetts Amherst. The authors have no declared conflict of interest.

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  1. Biopolymers and Colloids Research Laboratory, Department of Food Science, University of Massachusetts, Amherst, MA, 01003, USA

    Yan Li, Hang Xiao & David Julian McClements

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  1. Yan Li
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  2. Hang Xiao
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  3. David Julian McClements
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Correspondence to David Julian McClements.

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Li, Y., Xiao, H. & McClements, D.J. Encapsulation and Delivery of Crystalline Hydrophobic Nutraceuticals using Nanoemulsions: Factors Affecting Polymethoxyflavone Solubility. Food Biophysics 7, 341–353 (2012). https://doi.org/10.1007/s11483-012-9272-1

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  • DOI: https://doi.org/10.1007/s11483-012-9272-1

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