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Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization

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Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization

Auteurs : Yan Li ; Jinkai Zheng ; Hang Xiao ; David Julian Mcclements

Source :

Food hydrocolloids [ 0268-005X ] ; 2011.

RBID : PMC:3367464

Abstract

Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.

Url:

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3367464

DOI: 10.1016/j.foodhyd.2011.08.017
PubMed: 22685367
PubMed Central: 3367464

Affiliations:

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PMC:3367464

Le document en format XML

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<author><name sortKey="Li, Yan" sort="Li, Yan" uniqKey="Li Y" first="Yan" last="Li">Yan Li</name>
</author>
<author><name sortKey="Zheng, Jinkai" sort="Zheng, Jinkai" uniqKey="Zheng J" first="Jinkai" last="Zheng">Jinkai Zheng</name>
</author>
<author><name sortKey="Xiao, Hang" sort="Xiao, Hang" uniqKey="Xiao H" first="Hang" last="Xiao">Hang Xiao</name>
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<author><name sortKey="Mcclements, David Julian" sort="Mcclements, David Julian" uniqKey="Mcclements D" first="David Julian" last="Mcclements">David Julian Mcclements</name>
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<author><name sortKey="Zheng, Jinkai" sort="Zheng, Jinkai" uniqKey="Zheng J" first="Jinkai" last="Zheng">Jinkai Zheng</name>
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<front><div type="abstract" xml:lang="en"><p id="P1">Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (<italic>r</italic>
 < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.</p>
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  <front><journal-meta><journal-id journal-id-type="nlm-journal-id">8701770</journal-id>
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<title-group><article-title>Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization</article-title>
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<contrib-group><contrib contrib-type="author"><name><surname>Li</surname>
<given-names>Yan</given-names>
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<contrib contrib-type="author"><name><surname>Zheng</surname>
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<contrib contrib-type="author"><name><surname>Xiao</surname>
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<contrib contrib-type="author"><name><surname>McClements</surname>
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<aff id="A1">Biopolymers and Colloids Research Laboratory, Department of Food Science, University of Massachusetts, Amherst, Massachusetts 01003</aff>
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<author-notes><corresp id="CR1"><label>*</label>
Corresponding author: <email>mcclements@foodsci.umass.edu</email>
 Phone: 413-545-1019 Fax: 413-545-1262</corresp>
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<pub-date pub-type="nihms-submitted"><day>25</day>
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<month>9</month>
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<abstract><p id="P1">Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (<italic>r</italic>
 < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.</p>
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<kwd-group><kwd>Polymethoxyflavones</kwd>
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<funding-group><award-group><funding-source country="United States">National Cancer Institute : NCI</funding-source>
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Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization

Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization

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Abstract

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