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.