A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator

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Bibliographische Detailangaben
Zeitschriftentitel:	Cells
Personen und Körperschaften:	Manzo, Emiliano, Schiano Moriello, Aniello, Tinto, Francesco, Verde, Roberta, Allarà, Marco, De Petrocellis, Luciano, Pagano, Ester, Izzo, Angelo A., Di Marzo, Vincenzo, Petrosino, Stefania
In:	Cells, 10, 2021, 2, S. 450
Format:	E-Article
Sprache:	Englisch
veröffentlicht:	MDPI AG
Schlagwörter:	General Medicine

Details
Zusammenfassung:	<jats:p>Palmitoylethanolamide (PEA) is an endogenous anti-inflammatory lipid mediator and a widely used nutraceutical. In this study, we designed, realized, and tested a drug-carrier conjugate between PEA (the active drug) and glucuronic acid (the carrier). The conjugate, named GLUPEA, was characterized for its capability of increasing PEA levels and exerting anti-inflammatory activity both in vitro and in vivo. GLUPEA treatment, compared to the same concentration of PEA, resulted in higher cellular amounts of PEA and the endocannabinoid 2-arachidonoyl glycerol (2-AG), and increased 2-AG-induced transient receptor potential vanilloid type 1 (TRPV1) channel desensitization to capsaicin. GLUPEA inhibited pro-inflammatory monocyte chemoattractant protein 2 (MCP-2) release from stimulated keratinocytes, and it was almost as efficacious as ultra-micronized PEA at reducing colitis in dinitrobenzene sulfonic acid (DNBS)-injected mice when using the same dose. GLUPEA is a novel pro-drug able to efficiently mimic the anti-inflammatory and endocannabinoid enhancing actions of PEA.</jats:p>
Umfang:	450
ISSN:	2073-4409
DOI:	10.3390/cells10020450