Targeted delivery of atorvastatin via asialoglycoprotein receptor (ASGPR).
Bioorg Med Chem
; 27(11): 2187-2191, 2019 06 01.
Article
de En
| MEDLINE
| ID: mdl-31005367
ABSTRACT
Targeted drug delivery platforms can increase the concentration of drugs in specific cell populations, reduce adverse effects, and hence improve the therapeutic effect of drugs. Herein, we designed two conjugates by installing the targeting ligand GalNAc (N-acetylgalactosamine) onto atorvastatin (AT). Compared to the parent drug, these two conjugates, termed G2-AT and G2-K-AT, showed increased hepatic cellular uptake. Moreover, both conjugates were able to release atorvastatin, and consequently showed dramatic inhibition of ß-hydroxy-ß-methylglutaryl-CoA (HMG-CoA) reductase and increased LDL receptors on cell surface.
Mots clés
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Acétyl-galactosamine
/
Inhibiteurs de l'hydroxyméthylglutaryl-CoA réductase
/
Récepteurs des asialoglycoprotéines
/
Atorvastatine
Limites:
Animals
/
Humans
Langue:
En
Journal:
Bioorg Med Chem
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2019
Type de document:
Article
Pays d'affiliation:
Chine