Back to Journals » Drug Design, Development and Therapy » Volume 7

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

Authors Grillo SL, Keereetaweep J, Grillo MA, Chapman KD, Koulen P

Received 15 May 2013

Accepted for publication 13 June 2013

Published 12 August 2013 Volume 2013:7 Pages 747—752

DOI https://doi.org/10.2147/DDDT.S48324

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 4



Stephanie L Grillo,1,* Jantana Keereetaweep,2,* Michael A Grillo,1 Kent D Chapman,2 Peter Koulen1–3

1Vision Research Center, Department of Ophthalmology, School of Medicine, University of Missouri – Kansas City, Kansas City, MO, USA; 2University of North Texas, Center for Plant Lipid Research, Department of Biological Sciences, Denton, TX, USA; 3Department of Basic Medical Science, School of Medicine, University of Missouri – Kansas City, Kansas City, MO, USA

*These authors contributed equally to this work

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.

Keywords: cannabinoid receptor, vanilloid receptor, DBA/2 mice, lipid extraction, gas chromatography, mass spectrometry

Creative Commons License © 2013 The Author(s). This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.