SB431542-Loaded Liposomes Alleviate Liver Fibrosis by Suppressing TGF-β Signaling.
Animals
Benzamides
/ administration & dosage
Carbon Tetrachloride
/ adverse effects
Cell Line
Dioxoles
/ administration & dosage
Disease Models, Animal
Drug Liberation
Hepatic Stellate Cells
/ drug effects
Humans
Liposomes
Liver Cirrhosis, Experimental
/ chemically induced
Male
Mice
Mice, Inbred C57BL
Rats
Rats, Sprague-Dawley
Signal Transduction
/ drug effects
Tissue Distribution
Transforming Growth Factor beta
/ metabolism
SB431542
clinical application
hepatic stellate cells
liposome
liver fibrosis
Journal
Molecular pharmaceutics
ISSN: 1543-8392
Titre abrégé: Mol Pharm
Pays: United States
ID NLM: 101197791
Informations de publication
Date de publication:
02 11 2020
02 11 2020
Historique:
pubmed:
23
10
2020
medline:
15
9
2021
entrez:
22
10
2020
Statut:
ppublish
Résumé
Liver fibrosis is a common outcome of most chronic liver diseases, but there is no clinically approved drug for its treatment. Previous studies have reported the potential of SB431542 as an inhibitor of TGF-β signaling in the treatment of liver fibrosis, but it shows poor water solubility and low bioavailability. Here, we improve these characteristics of SB431542 by loading it into liposomes (SB-Lips) with two FDA-approved excipients: soya phosphatidyl S100 and Solutol HS15.
Identifiants
pubmed: 33089693
doi: 10.1021/acs.molpharmaceut.0c00633
doi:
Substances chimiques
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide
0
Benzamides
0
Dioxoles
0
Liposomes
0
Transforming Growth Factor beta
0
Carbon Tetrachloride
CL2T97X0V0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM