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

Content Provider	PubMed Central
Author	Grillo, Stephanie L. Keereetaweep, Jantana Grillo, Michael A. Chapman, Kent D. Peter, Koulen
Copyright Year	2013
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.
Related Links	http://dx.doi.org/10.2147/DDDT.S48324
Ending Page	752
Page Count	6
Starting Page	747
File Format	PDF
ISSN	11778881
e-ISSN	11778881
Journal	Drug Design, Development and Therapy
Volume Number	7
Language	English
Publisher	Dove Medical Press
Publisher Date	2013-08-12
Access Restriction	Open
Rights Holder	Dove Medical Press
Subject Keyword	Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Pharmacology Pharmaceutical Science

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