Celastrol-loaded PEG-b-PPS nanocarriers as an anti-inflammatory treatment for atherosclerosis.
Biomater Sci
; 7(2): 657-668, 2019 Jan 29.
Article
em En
| MEDLINE
| ID: mdl-30601470
ABSTRACT
In this work, the hydrophobic small molecule NF-κB inhibitor celastrol was loaded into poly(ethylene glycol)-b-poly(propylene sulfide) (PEG-b-PPS) micelles. PEG-b-PPS micelles demonstrated high loading efficiency, low polydispersity, and no morphological changes upon loading with celastrol. Encapsulation of celastrol within these nanocarriers significantly reduced cytotoxicity compared to free celastrol, while simultaneously expanding the lower concentration range for effective inhibition of NF-κB signaling by nearly 50 000-fold. Furthermore, celastrol-loaded micelles successfully reduced TNF-α secretion after LPS stimulation of RAW 264.7 cells and reduced the number of neutrophils and inflammatory monocytes within atherosclerotic plaques of ldlr-/- mice. This reduction in inflammatory cells was matched by a reduction in plaque area, suggesting that celastrol-loaded nanocarriers may serve as an anti-inflammatory treatment for atherosclerosis.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Polietilenoglicóis
/
Sulfetos
/
Triterpenos
/
Portadores de Fármacos
/
Anti-Inflamatórios não Esteroides
/
Placa Aterosclerótica
Limite:
Animals
Idioma:
En
Revista:
Biomater Sci
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Estados Unidos