15d-PGJ2-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation

PLoS One. 2016 Aug 30;11(8):e0161796. doi: 10.1371/journal.pone.0161796. eCollection 2016.

Abstract

15-deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2), a peroxisome proliferator-activated 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.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • BALB 3T3 Cells
  • Carrageenan / adverse effects
  • Cell Survival / drug effects
  • Gene Expression Regulation / drug effects
  • Interleukins / genetics*
  • Lipopolysaccharides / adverse effects
  • Mice
  • Mice, Inbred BALB C
  • Nanoparticles / chemistry
  • Neutrophil Infiltration / drug effects*
  • Particle Size
  • Peritonitis / chemically induced
  • Peritonitis / drug therapy*
  • Peritonitis / immunology
  • Prostaglandin D2 / administration & dosage
  • Prostaglandin D2 / analogs & derivatives*
  • Prostaglandin D2 / chemistry
  • Prostaglandin D2 / pharmacology

Substances

  • 15-deoxyprostaglandin J2
  • Anti-Inflammatory Agents
  • Interleukins
  • Lipopolysaccharides
  • Carrageenan
  • Prostaglandin D2

Grants and funding

The authors gratefully acknowledge financial support from the Brazilian funding agencies São Paulo Research Foundation (FAPESP) and National Council for Scientific and Technological Development (CNPq). NFSM was supported by a research fellowship grant# 2014/11016-8, São Paulo Research Foundation. MHN was supported by a research fellowship grant # 303555/2013-0 (CNPq).