Cargando…
15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation
15-deoxy-Δ(12,14)-prostaglandin J(2) (15d-PGJ(2)), 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 therapeu...
Autores principales: | , , , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2016
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5004889/ https://www.ncbi.nlm.nih.gov/pubmed/27575486 http://dx.doi.org/10.1371/journal.pone.0161796 |
_version_ | 1782450836495925248 |
---|---|
author | de Melo, Nathalie Ferreira Silva de Macedo, Cristina Gomes Bonfante, Ricardo Abdalla, Henrique Ballassini da Silva, Camila Morais Gonçalves Pasquoto, Tatiane de Lima, Renata Fraceto, Leonardo Fernandes Clemente-Napimoga, Juliana Trindade Napimoga, Marcelo Henrique |
author_facet | de Melo, Nathalie Ferreira Silva de Macedo, Cristina Gomes Bonfante, Ricardo Abdalla, Henrique Ballassini da Silva, Camila Morais Gonçalves Pasquoto, Tatiane de Lima, Renata Fraceto, Leonardo Fernandes Clemente-Napimoga, Juliana Trindade Napimoga, Marcelo Henrique |
author_sort | de Melo, Nathalie Ferreira Silva |
collection | PubMed |
description | 15-deoxy-Δ(12,14)-prostaglandin J(2) (15d-PGJ(2)), 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-PGJ(2)-SLN was therefore developed and investigated in terms of its immunomodulatory potential. 15d-PGJ(2)-SLN and unloaded SLN were physicochemically characterized and experiments in vivo were performed. Animals were pretreated with 15d-PGJ(2)-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-PGJ(2)-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-PGJ(2)-SLN formulation was able to reduce neutrophil migration in three inflammation models tested using low concentrations of 15d-PGJ(2). Additionally, 15d-PGJ(2)-SLN increased IL-10 levels and reduced IL-1β as well as IL-17 in peritoneal fluid. The new 15d-PGJ(2)-SLN formulation highlights perspectives of a potent anti-inflammatory system using low concentrations of 15d-PGJ(2). |
format | Online Article Text |
id | pubmed-5004889 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-50048892016-09-12 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation de Melo, Nathalie Ferreira Silva de Macedo, Cristina Gomes Bonfante, Ricardo Abdalla, Henrique Ballassini da Silva, Camila Morais Gonçalves Pasquoto, Tatiane de Lima, Renata Fraceto, Leonardo Fernandes Clemente-Napimoga, Juliana Trindade Napimoga, Marcelo Henrique PLoS One Research Article 15-deoxy-Δ(12,14)-prostaglandin J(2) (15d-PGJ(2)), 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-PGJ(2)-SLN was therefore developed and investigated in terms of its immunomodulatory potential. 15d-PGJ(2)-SLN and unloaded SLN were physicochemically characterized and experiments in vivo were performed. Animals were pretreated with 15d-PGJ(2)-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-PGJ(2)-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-PGJ(2)-SLN formulation was able to reduce neutrophil migration in three inflammation models tested using low concentrations of 15d-PGJ(2). Additionally, 15d-PGJ(2)-SLN increased IL-10 levels and reduced IL-1β as well as IL-17 in peritoneal fluid. The new 15d-PGJ(2)-SLN formulation highlights perspectives of a potent anti-inflammatory system using low concentrations of 15d-PGJ(2). Public Library of Science 2016-08-30 /pmc/articles/PMC5004889/ /pubmed/27575486 http://dx.doi.org/10.1371/journal.pone.0161796 Text en © 2016 de Melo et al http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/) , which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
spellingShingle | Research Article de Melo, Nathalie Ferreira Silva de Macedo, Cristina Gomes Bonfante, Ricardo Abdalla, Henrique Ballassini da Silva, Camila Morais Gonçalves Pasquoto, Tatiane de Lima, Renata Fraceto, Leonardo Fernandes Clemente-Napimoga, Juliana Trindade Napimoga, Marcelo Henrique 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title | 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title_full | 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title_fullStr | 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title_full_unstemmed | 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title_short | 15d-PGJ(2)-Loaded Solid Lipid Nanoparticles: Physicochemical Characterization and Evaluation of Pharmacological Effects on Inflammation |
title_sort | 15d-pgj(2)-loaded solid lipid nanoparticles: physicochemical characterization and evaluation of pharmacological effects on inflammation |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5004889/ https://www.ncbi.nlm.nih.gov/pubmed/27575486 http://dx.doi.org/10.1371/journal.pone.0161796 |
work_keys_str_mv | AT demelonathalieferreirasilva 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT demacedocristinagomes 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT bonfantericardo 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT abdallahenriqueballassini 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT dasilvacamilamoraisgoncalves 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT pasquototatiane 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT delimarenata 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT fracetoleonardofernandes 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT clementenapimogajulianatrindade 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation AT napimogamarcelohenrique 15dpgj2loadedsolidlipidnanoparticlesphysicochemicalcharacterizationandevaluationofpharmacologicaleffectsoninflammation |