Polymer-ritonavir derivate nanomedicine with pH-sensitive activation possesses potent anti-tumor activity in vivo via inhibition of proteasome and STAT3 signaling.
Antitumor activity
Polymer carrier
Proteasome inhibition
Ritonavir derivate
STAT3 signaling inhibition
pH-controlled release
Journal
Journal of controlled release : official journal of the Controlled Release Society
ISSN: 1873-4995
Titre abrégé: J Control Release
Pays: Netherlands
ID NLM: 8607908
Informations de publication
Date de publication:
10 04 2021
10 04 2021
Historique:
received:
11
11
2020
revised:
07
03
2021
accepted:
10
03
2021
pubmed:
17
3
2021
medline:
8
7
2021
entrez:
16
3
2021
Statut:
ppublish
Résumé
Drug repurposing is a promising strategy for identifying new applications for approved drugs. Here, we describe a polymer biomaterial composed of the antiretroviral drug ritonavir derivative (5-methyl-4-oxohexanoic acid ritonavir ester; RD), covalently bound to HPMA copolymer carrier via a pH-sensitive hydrazone bond (P-RD). Apart from being more potent inhibitor of P-glycoprotein in comparison to ritonavir, we found RD to have considerable cytostatic activity in six mice (IC
Identifiants
pubmed: 33722611
pii: S0168-3659(21)00126-7
doi: 10.1016/j.jconrel.2021.03.015
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Polymers
0
Doxorubicin
80168379AG
Proteasome Endopeptidase Complex
EC 3.4.25.1
Ritonavir
O3J8G9O825
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
563-580Informations de copyright
Copyright © 2021 Elsevier B.V. All rights reserved.