N-Palmitoylethanolamine depot injection increased its tissue levels and those of other acylethanolamide lipids

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Article discussing how the N-palmitoylethanolamine depot injection increased its tissue levels and those of other acylethanolamide lipids.

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6 p.

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Grillo, Stephanie L.; Keereetaweep, Jantana; Grillo, Michael A.; Chapman, Kent D. & Koulen, Peter August 12, 2013.

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Article discussing how the N-palmitoylethanolamine depot injection increased its tissue levels and those of other acylethanolamide lipids.

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6 p.

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Abstract: N-Palmitoylethanolamine (NAE 16:0) is an endogenous lipid signaling molecule that has limited water solubility, and its action is short-lived due to its rapid metabolism. This poses a problem for use in vivo as oral administration requires a high concentration for significant levels to reach target tissues, and injection of the compound in a dimethyl sulfoxide- or ethanol-based vehicle is usually not desirable during long-term treatment. A depot injection of NAE 16:0 was successfully emulsified in sterile corn oil (10 mg/kg) and administered in young DBA/2 mice in order to elevate baseline levels of NAE 16:0 in target tissues. NAE 16:0 levels were increased in various tissues, particularly in the retina, 24 and 48 hours following injections. Increases ranged between 22% and 215% (above basal levels) in blood serum, heart, brain, and retina and induced an entourage effect by increasing levels of other 18 carbon N-Acylethanolamines (NAEs), which ranged between 31% and 117% above baseline. These results indicate that NAE 16:0 can be used as a depot preparation, avoiding the use of inadequate vehicles, and can provide the basis for designing tissue-specific dosing regimens for therapies involving NAEs and related compounds.

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  • Drug Design, Development and Therapy, 2013(7), Dove Medical Press Ltd, August 12, 2013, pp. 1-6

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  • Publication Title: Drug Design, Development and Therapy
  • Volume: 2013
  • Issue: 7
  • Page Start: 747
  • Page End: 752
  • Peer Reviewed: Yes

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  • August 12, 2013

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  • March 14, 2014, 8:48 a.m.

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  • Nov. 28, 2023, 10:57 a.m.

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Grillo, Stephanie L.; Keereetaweep, Jantana; Grillo, Michael A.; Chapman, Kent D. & Koulen, Peter. N-Palmitoylethanolamine depot injection increased its tissue levels and those of other acylethanolamide lipids, article, August 12, 2013; [Princeton, New Jersey]. (https://digital.library.unt.edu/ark:/67531/metadc277295/: accessed December 9, 2023), University of North Texas Libraries, UNT Digital Library, https://digital.library.unt.edu; crediting UNT College of Arts and Sciences.

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