Abstract
FMOC-isocyclosporine A, a fluorescent labeled cyclosporine A, was encapsulated in solid lipid nanoparticles (SLN) prepared by the coacervation technique, and its anti-inflammatory activity was evaluated. The anti-inflammatory activity of the fluorescent labelled molecule, measured as inhibition of TNF-α secretion, is similar to the native one. SLN were compared to commercial formulations, through measurement of cytokine release and drug uptake in rat peripheral blood mononuclear cells. Drug-loaded SLN inhibit TNF-α secretion in a lower extent than commercial formulations, probably due to a lower uptake by the cells, but the increase of IL-10 secretion caused by the lipid matrix itself makes this formulation interesting for its anti-inflammatory activity.
Keywords: Coacervation, cyclosporine A, cytokines, FMOC, inflammation, solid lipid nanoparticles.
Protein & Peptide Letters
Title:Solid Lipid Nanoparticles Loaded with Fluorescent-labelled Cyclosporine A: Anti-Inflammatory Activity In Vitro
Volume: 21 Issue: 11
Author(s): Marina Gallarate, Loredana Serpe, Federica Foglietta, Gian Paolo Zara, Susanna Giordano, Elena Peira, Daniela Chirio and Luigi Battaglia
Affiliation:
Keywords: Coacervation, cyclosporine A, cytokines, FMOC, inflammation, solid lipid nanoparticles.
Abstract: FMOC-isocyclosporine A, a fluorescent labeled cyclosporine A, was encapsulated in solid lipid nanoparticles (SLN) prepared by the coacervation technique, and its anti-inflammatory activity was evaluated. The anti-inflammatory activity of the fluorescent labelled molecule, measured as inhibition of TNF-α secretion, is similar to the native one. SLN were compared to commercial formulations, through measurement of cytokine release and drug uptake in rat peripheral blood mononuclear cells. Drug-loaded SLN inhibit TNF-α secretion in a lower extent than commercial formulations, probably due to a lower uptake by the cells, but the increase of IL-10 secretion caused by the lipid matrix itself makes this formulation interesting for its anti-inflammatory activity.
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Gallarate Marina, Serpe Loredana, Foglietta Federica, Zara Paolo Gian, Giordano Susanna, Peira Elena, Chirio Daniela and Battaglia Luigi, Solid Lipid Nanoparticles Loaded with Fluorescent-labelled Cyclosporine A: Anti-Inflammatory Activity In Vitro, Protein & Peptide Letters 2014; 21 (11) . https://dx.doi.org/10.2174/0929866521666140806164410
DOI https://dx.doi.org/10.2174/0929866521666140806164410 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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