Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers.
Biol Pharm Bull
; 43(9): 1301-1305, 2020.
Article
em En
| MEDLINE
| ID: mdl-32879203
ABSTRACT
Enhancing blood flow to tumors is a prominent strategy for improving the tumor accumulation of macromolecular drugs through the enhanced permeability and retention (EPR) effect. IRL-1620 is an agonist of the endothelin B receptor, and is a promising molecule to enhance tumor blood flow by activating endothelial nitric oxide synthase. However, contradictory effects on tumor blood flow modulation have been reported because the effects of IRL-1620 may differ in different animal models. Here, we examined for the first time the effect of IRL-1620 on the EPR effect for PEGylated liposomes in a CT-26 murine colon cancer model. Co-injection of IRL-1620 at an optimum dose (3 nmol/kg) nearly doubled the tumor accumulation of liposomes compared with controls, indicating that IRL-1620 enhanced the EPR effect in the present colon cancer model. Co-injection of IRL-1620 is a promising strategy to improve the therapeutic effects of macromolecular drugs while reducing their side effects.
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Base de dados:
MEDLINE
Assunto principal:
Fragmentos de Peptídeos
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Protocolos de Quimioterapia Combinada Antineoplásica
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Endotelinas
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Neoplasias do Colo
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Antagonistas do Receptor de Endotelina B
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article