Preparation and protective effects of 1,8-cineole-loaded self-microemulsifying drug delivery system on lipopolysaccharide-induced endothelial injury in mice.
Eur J Pharm Sci
; 127: 14-23, 2019 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-30336203
ABSTRACT
An optimised 1,8-cineole-loaded self-microemulsifying drug delivery system (CIN-SMEDDS) with a mean droplet size, polydispersity index, mean zeta potential and encapsulation efficiency of 38.14⯱â¯1.47â¯nm, 0.208⯱â¯0.036, -9.312⯱â¯1.764â¯mV and 95.35%⯱â¯1.13%, respectively, successfully ameliorated the lipopolysaccharide (LPS)-induced endothelial injury in mice. Acute toxicity assay in mice through the oral administration of CIN-SMEDDS showed that the median lethal dose of CIN-SMEDDS was 2998.9â¯mg/kg. The results of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay indicated that the cytotoxicity of CIN-SMEDDS to Caco-2 cells may be ascribed to the surfactant/co-surfactant mixture. In particular, CIN-SMEDDS remarkably inhibited inflammatory cytokines IL-1ß, IL-6 and IL-8 with a simultaneous increase in IL-10 in LPS-treated mice. Haematoxylin-eosin staining results showed that CIN-SMEDDS attenuated LPS-induced vascular endothelial injury. Western blot results showed that the vascular protective effects of CIN-SMEDDS were associated with the NF-κB and peroxisome proliferator-activated receptor γ signalling pathways. These findings indicated that CIN-SMEDDS can attenuate LPS-induced endothelial injury and thus was proposed as a promising agent for the treatment of inflammatory cardiovascular disease.
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MEDLINE
Assunto principal:
Aorta Torácica
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Substâncias Protetoras
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Eucaliptol
Limite:
Animals
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Female
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Humans
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Male
Idioma:
En
Revista:
Eur J Pharm Sci
Assunto da revista:
FARMACIA
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FARMACOLOGIA
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QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article