15d-PGJ2-loaded solid lipid nanoparticles: Physicochemical characterization and evaluation of pharmacological effects on inflammation
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2016-08-01
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De Melo, Nathalie Ferreira Silva [UNESP]
De Macedo, Cristina Gomes
Bonfante, Ricardo
Abdalla, Henrique Ballassini
Da Silva, Camila Morais Gon�alves
Pasquoto, Tatiane
De Lima, Renata
Fraceto, Leonardo Fernandes [UNESP]
Clemente-Napimoga, Juliana Trindade
Napimoga, Marcelo Henrique
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15-deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2), a peroxisome proliferator-ctivated receptor-γ (PPAR-γ) agonist, has physiological properties including pronounced anti-inflammatory activity, though it binds strongly to serum albumin. The use of solid lipid nanoparticles (SLN) can improve therapeutic properties increasing drug efficiency and availability. 15d-PGJ2-SLN was therefore developed and investigated in terms of its immunomodulatory potential. 15d-PGJ2-SLN and unloaded SLN were physicochemically characterized and experiments in vivo were performed. Animals were pretreated with 15d-PGJ2-SLN at concentrations of 3, 10 or 30 μg�kg-1 before inflammatory stimulus with carrageenan (Cg), lipopolysaccharide (LPS) or mBSA (immune response). Interleukins (IL-1β, IL-10 and IL-17) levels were also evaluated in exudates. The 15d-PGJ2-SLN system showed good colloidal parameters and encapsulation efficiency of 96%. The results showed that the formulation was stable for up to 120 days with low hemolytic effects. The 15d-PGJ2-SLN formulation was able to reduce neutrophil migration in three inflammation models tested using low concentrations of 15d-PGJ2. Additionally, 15d-PGJ2-SLN increased IL-10 levels and reduced IL-1β as well as IL-17 in peritoneal fluid. The new 15d-PGJ2-SLN formulation highlights perspectives of a potent anti-inflammatory system using low concentrations of 15d-PGJ2.
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PLoS ONE, v. 11, n. 8, 2016.