Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain
Palmitoylethanolamide (PEA), a fatty acid amide, has been widely investigated for its analgesic and anti-inflammatory properties. The ultra-micronized formulation of PEA (um-PEA), that has an enhanced rate of dissolution, is extensively used. Acetyl-<span style="font-variant: small-caps;&quo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-02-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/4/1967 |
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| author | Alessio Ardizzone Roberta Fusco Giovanna Casili Marika Lanza Daniela Impellizzeri Emanuela Esposito Salvatore Cuzzocrea |
| author_facet | Alessio Ardizzone Roberta Fusco Giovanna Casili Marika Lanza Daniela Impellizzeri Emanuela Esposito Salvatore Cuzzocrea |
| author_sort | Alessio Ardizzone |
| collection | DOAJ |
| description | Palmitoylethanolamide (PEA), a fatty acid amide, has been widely investigated for its analgesic and anti-inflammatory properties. The ultra-micronized formulation of PEA (um-PEA), that has an enhanced rate of dissolution, is extensively used. Acetyl-<span style="font-variant: small-caps;">l</span>-carnitine (LAC), employed for the treatment of neuropathic pain in humans, is able to cause analgesia by up-regulating type-2 metabotropic glutamate (mGlu2) receptors. In the present study, we tested different associations of um-PEA, LAC and non-micronized PEA (non-m-PEA) in a rat model of carrageenan (CAR)-induced paw edema. Intraplantar injection of CAR into the hind paw of animals caused edema, thermal hyperalgesia, accumulation of infiltrating inflammatory cells and augmented myeloperoxidase (MPO) activity. All these parameters were decreased in a significantly manner by oral administration of a compound constituted by a mixture of um-PEA and LAC in relation 1:1 (5 mg/kg), but not with the association of single compounds administered one after the other. These findings showed the superior anti-inflammatory and anti-nociceptive action displayed by oral administration of um-PEA and LAC versus LAC plus, separate but consecutive, um-PEA in the rat paw CAR model of inflammatory pain. |
| first_indexed | 2024-03-09T00:48:37Z |
| format | Article |
| id | doaj.art-702fe88b1cca4054af1b725c95d72374 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T00:48:37Z |
| publishDate | 2021-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-702fe88b1cca4054af1b725c95d723742023-12-11T17:21:05ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-02-01224196710.3390/ijms22041967Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory PainAlessio Ardizzone0Roberta Fusco1Giovanna Casili2Marika Lanza3Daniela Impellizzeri4Emanuela Esposito5Salvatore Cuzzocrea6Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), ItalyPalmitoylethanolamide (PEA), a fatty acid amide, has been widely investigated for its analgesic and anti-inflammatory properties. The ultra-micronized formulation of PEA (um-PEA), that has an enhanced rate of dissolution, is extensively used. Acetyl-<span style="font-variant: small-caps;">l</span>-carnitine (LAC), employed for the treatment of neuropathic pain in humans, is able to cause analgesia by up-regulating type-2 metabotropic glutamate (mGlu2) receptors. In the present study, we tested different associations of um-PEA, LAC and non-micronized PEA (non-m-PEA) in a rat model of carrageenan (CAR)-induced paw edema. Intraplantar injection of CAR into the hind paw of animals caused edema, thermal hyperalgesia, accumulation of infiltrating inflammatory cells and augmented myeloperoxidase (MPO) activity. All these parameters were decreased in a significantly manner by oral administration of a compound constituted by a mixture of um-PEA and LAC in relation 1:1 (5 mg/kg), but not with the association of single compounds administered one after the other. These findings showed the superior anti-inflammatory and anti-nociceptive action displayed by oral administration of um-PEA and LAC versus LAC plus, separate but consecutive, um-PEA in the rat paw CAR model of inflammatory pain.https://www.mdpi.com/1422-0067/22/4/1967palmitoylethanolamide (PEA)acetyl-<span style="font-variant: small-caps">l</span>-carnitine (LAC)carrageenan (CAR)edemainflammatory pain |
| spellingShingle | Alessio Ardizzone Roberta Fusco Giovanna Casili Marika Lanza Daniela Impellizzeri Emanuela Esposito Salvatore Cuzzocrea Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain International Journal of Molecular Sciences palmitoylethanolamide (PEA) acetyl-<span style="font-variant: small-caps">l</span>-carnitine (LAC) carrageenan (CAR) edema inflammatory pain |
| title | Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain |
| title_full | Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain |
| title_fullStr | Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain |
| title_full_unstemmed | Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain |
| title_short | Effect of Ultra-Micronized-Palmitoylethanolamide and Acetyl-<span style="font-variant: small-caps">l</span>-Carnitine on Experimental Model of Inflammatory Pain |
| title_sort | effect of ultra micronized palmitoylethanolamide and acetyl span style font variant small caps l span carnitine on experimental model of inflammatory pain |
| topic | palmitoylethanolamide (PEA) acetyl-<span style="font-variant: small-caps">l</span>-carnitine (LAC) carrageenan (CAR) edema inflammatory pain |
| url | https://www.mdpi.com/1422-0067/22/4/1967 |
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