POSSIBLE “ENTOURAGE” EFFECT OF PALMITOYLETHANOLAMIDE IN DOG AND HUMAN PLASMA (Comunicazione a convegno)

Type
Label
  • POSSIBLE “ENTOURAGE” EFFECT OF PALMITOYLETHANOLAMIDE IN DOG AND HUMAN PLASMA (Comunicazione a convegno) (literal)
Anno
  • 2010-01-01T00:00:00+01:00 (literal)
Alternative label
  • Stefania Petrosino, Pilar Brazis, Anna Puigdemont, Mariella Fusco, Francesca Comelli, Barbara Costa and Vincenzo Di Marzo, (2010)
    POSSIBLE “ENTOURAGE” EFFECT OF PALMITOYLETHANOLAMIDE IN DOG AND HUMAN PLASMA
    in ICRS 20th Symposium, Lund, Sweden
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Stefania Petrosino, Pilar Brazis, Anna Puigdemont, Mariella Fusco, Francesca Comelli, Barbara Costa and Vincenzo Di Marzo, (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#descrizioneSinteticaDelProdotto
  • Introduction: Palmitoylethanolamide (PEA) has emerged recently as an important local pro-homeostatic mediator that can be also administered exogenously as the active principle of anti-inflammatory and analgesic preparations. Several mechanisms have been proposed to explain these effects of PEA. One of these is the “entourage effect” on the tissue levels or CB1-, CB2- or TRPV1-mediated effects of endocannabinoids. Here we have studied the plasma bioavailability of an acute oral administration of PEA to either dogs or humans and its effects on plasma endocannabinoid levels. Methods: Four Beagle dogs spontaneously hypersensitive to Ascaris suum, with mean body weights of 14.0±0.6 kg were used in this study. The animals were fasted overnight before per os administration of ultra-micronized PEA (30 mg/kg). Ten fasted healthy human volunteers (4M/6F, age 43±7, mean body weight 73±12) were also recruited and administered with either 300 or 1200 mg (2x600 mg/tablet) of ultra-micronized PEA, after giving informed consent. In dogs, blood sample collection was carried out before administration of PEA (T0), and 1 (T1), 2 (T2), 4 (T4) and 8 (T8) hours after administration. In human volunteers, instead, blood sample collection was carried out before (T0), and after 2 (T2), 4 (T4) and 6 (T6) hours after administration of PEA, in the experiment with 300 mg of the compound; and before (T0), and 1 (T1), 2 (T2), 4 (T4) and 6 (T6) hours after administration of PEA, in the experiment with the 1200 mg dose. After blood sample collection, plasma lipids were extracted, pre-purified on silica gel and submitted to isotope dilution LC-MS analysis for anandamide (AEA), 2-arachidonoylglycerol (2-AG), PEA and oleoylethanolamide (OEA). Results: In dogs, a significant 6-fold elevation of PEA plasma levels vs. T0 was observed at T1 and T2, accompanied by a strong (15-20-fold) elevation of 2-AG, but not AEA or OEA, levels. Both PEA and 2-AG levels returned to normal between T4 and T8. In healthy volunteers, PEA plasma levels were increased 2-fold at T2 with 300 mg PEA, whereas 2-AG levels were slightly reduced at T2, and enhanced between T4 and T6 vs. T0. PEA plasma levels were strongly increased (9-fold) at both T1 and T2 with the higher dose of 1200 mg, and in this case 2-AG levels were slightly increased only at T6 vs. T0. No changes were observed at any time or dose for AEA and OEA levels. Conclusions: This is the first demonstration that orally administered PEA reaches the bloodstream in dogs and human subjects, and that PEA elevates circulating 2-AG levels. The stronger and more rapid “entourage” effect of PEA observed in dogs, compared to healthy patients, might be due to the former being sensitised to allergic reactions to A. suum, or to the more favourable bioavailability of PEA in this species. Acknowledgments: This study was supported by Epitech Group S.r.l. and Innovet Italia S.r.l. (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • 1Endocannabinoid Research Group, Institute of Biomolecular Chemistry, CNR, Pozzuoli, NA, Italy; 2UNIVET. Spain; 3Dept Farmacología, Universitat Autònoma de Barcelona, Spain ; 4Epitech Group S.r.l., Padova, Italy; 5Department of Biotechnology and Bioscience, University of Milano-Bicocca, Milano, Italy (literal)
Titolo
  • POSSIBLE “ENTOURAGE” EFFECT OF PALMITOYLETHANOLAMIDE IN DOG AND HUMAN PLASMA (literal)
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