title: Nanoparticles prolong N-palmitoylethanolamide anti-inflammatory and analgesic effects in vivo.
abstract: N-Palmitoylethanolamide showed great therapeutic potential in the treatment of inflammation and pain but its unfavourable pharmacokinetics properties will hinder its use in the clinical practice. A nanotechnology-based formulation was developed to enhance the probability of N-palmitoylethanolamide therapeutic success, especially in skin disease management. Lipid nanoparticles were produced and characterized to evaluate their mean size, ζ-potential, thermal behaviour, and morphology. The ability of N-palmitoylethanolamide to diffuse across the epidermis as well as anti-inflammatory and analgesic effects were investigated. Particles had a mean size of about 150 nm and a ζ-potential of -40 mV. DSC data confirmed the solid state of the matrix and the embedding of N-palmitoylethanolamide while electron microscopy have evidenced a peculiar internal structure (i.e., low-electrondense spherical objects within the matrix) that can be reliably ascribed to the presence of oil nanocompartments. Lipid nanoparticles increased N-palmitoylethanolamide percutaneous diffusion and prolonged the anti-inflammatory and analgesic effects in vivo. Lipid nanoparticles seem a good nanotechnology-based strategy to bring N-palmitoylethanolamide to clinics.
authors: Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano (SA), Italy.
authors: Diana
authors: D
authors: Tronino
authors: Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
authors: Alessia
authors: A
authors: Offerta
authors: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy.
authors: Carmine
authors: C
authors: Ostacolo
authors: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy.
authors: Roberto
authors: R
authors: Russo
authors: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy.
authors: Carmen
authors: C
authors: De Caro
authors: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy.
authors: Antonio
authors: A
authors: Calignano
authors: Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Viale Andrea Doria 6, 95125 Catania, Italy. Electronic address: capuglia@unict.it.
authors: Carmelo
authors: C
authors: Puglia
authors: Scuola di Scienze del Farmaco e dei Prodotti della Salute, Università degli Studi di Camerino, Piazza dei Costanti, 62032 Camerino, Italy. Electronic address: paolo.blasi@unicam.it.
authors: Paolo
authors: P
authors: Blasi
mesh_terms: D000328:Adult; D000577:Amides; D000700:Analgesics / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control*; D004817:Epidermis / Q000378:metabolism; D004983:Ethanolamines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D005121:Extremities / Q000473:pathology; D006801:Humans; D006930:Hyperalgesia / Q000517:prevention & control*; D008297:Male; D051379:Mice; D046529:Microscopy, Electron, Transmission; D008875:Middle Aged; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010169:Palmitic Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D010316:Particle Size; D012869:Skin Absorption
chemical_list: D000577:Amides; D000700:Analgesics; D000893:Anti-Inflammatory Agents; D004983:Ethanolamines; D010169:Palmitic Acids; C005958:palmidrol; D002351:Carrageenan
keywords: Analgesia; Inflammation; N-Palmitoylethanolamide; Nanoparticles; Nanostructured lipid carriers; Percutaneous absorption