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Galactosyl prodrug of palmitoylethanolamide: Synthesis, stability, cell permeation and cytoprotective activity

Luongo, Elvira and Russo, Roberto and Avagliano, Carmen and Santoro, Anna and Melisi, Daniela and Orefice, Nicola Salvatore and Mattace Raso, Giuseppina and Meli, Rosaria and Magliocca, Salvatore and Nieddu, Maria and Pinheiro Santiago, Gilvandete Maria and Boatto, Gianpiero and Calignano, Antonio and Rimoli, Maria Grazia (2014) Galactosyl prodrug of palmitoylethanolamide: Synthesis, stability, cell permeation and cytoprotective activity. European Journal of Pharmaceutical Sciences, Vol. 62 , p. 33-39. ISSN 0928-0987. Article.

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DOI: 10.1016/j.ejps.2014.05.009


N-Palmitoylethanolamide (PEA) is emerging as a novel therapeutic agent in the treatment of neuropathic pain and neurodegenerative diseases. Unfortunately, PEA poorly reaches the central nervous system (CNS), after peripheral administration, since it is inactivated through intracellular hydrolysis by lipid amidases. Since prodrug approach is one of the most popular methods used to increase cell permeability, the aim of this paper consists in the synthesis of a new galactosyl prodrug of PEA, the palmitoylethanolamide-succinamyl-D-galactos-6′-yl ester (PEAGAL). Biological experiments both in neuroblastoma and in C6 glioma cells, together with quantitative analyses performed through a LC-MS-MS technique, demonstrate the better efficacy of PEAGAL compared to PEA and its higher cell permeation. Our results encourage further experiments in animal models of neuropathic pain and of neurological disorders and/or neurodegenerative diseases, in order to promote a more effective peripherally administrated derivative of PEA.

Item Type:Article
ID Code:9981
Uncontrolled Keywords:Cell culture, cytoprotection, liquid chromatography, N-palmitoylethanolamide, permeability, prodrugs
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier Science
Deposited On:21 Jul 2014 17:09

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