Nanoparticles prolong N-palmitoylethanolamide anti-inflammatory and analgesic effects in vivo

[Display omitted] •Nanoparticles were prepared with a binary mixture of lipids.•Electron microscopy evidenced low-electrondense spherical objects within nanoparticle matrix ascribed to oil nanocompartments.•Lipid nanoparticles increase N-palmitoylethanolamide percutaneous absorption.•Nanoparticles p...

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Bibliographic Details
Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2016-05, Vol.141, p.311-317
Main Authors: Tronino, Diana, Offerta, Alessia, Ostacolo, Carmine, Russo, Roberto, De Caro, Carmen, Calignano, Antonio, Puglia, Carmelo, Blasi, Paolo
Format: Article
Language:English
Subjects:
Adult
Analgesia
Analgesics - chemistry
Analgesics - pharmacokinetics
Analgesics - pharmacology
Animals
Anti-Inflammatory Agents - chemistry
Anti-Inflammatory Agents - pharmacokinetics
Anti-Inflammatory Agents - pharmacology
Calorimetry, Differential Scanning
Carrageenan
Edema - chemically induced
Edema - prevention & control
Epidermis - metabolism
Ethanolamines - chemistry
Ethanolamines - pharmacokinetics
Ethanolamines - pharmacology
Extremities - pathology
Humans
Hyperalgesia - prevention & control
Inflammation
Male
Mice
Microscopy, Electron, Transmission
Middle Aged
N-Palmitoylethanolamide
Nanoparticles
Nanoparticles - chemistry
Nanoparticles - ultrastructure
Nanostructured lipid carriers
Palmitic Acids - chemistry
Palmitic Acids - pharmacokinetics
Palmitic Acids - pharmacology
Particle Size
Percutaneous absorption
Skin Absorption
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Summary:[Display omitted] •Nanoparticles were prepared with a binary mixture of lipids.•Electron microscopy evidenced low-electrondense spherical objects within nanoparticle matrix ascribed to oil nanocompartments.•Lipid nanoparticles increase N-palmitoylethanolamide percutaneous absorption.•Nanoparticles prolonged N-palmitoylethanolamide anti-inflammatory and analgesic effects in vivo. 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 150nm and a ζ-potential of −40mV. 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.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2016.01.058