Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers

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  • Feng Haitao
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University
  • Nam Le Thanh
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University
  • Yoshikawa Takuma
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University
  • Kishimura Akihiro
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University Graduate School of System Life Science, Kyushu University International Research Center for Molecular Systems, Kyushu University
  • Mori Takeshi
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University Graduate School of System Life Science, Kyushu University
  • Katayama Yoshiki
    Department of Applied Chemistry, Faculty of Engineering, Kyushu University Graduate School of System Life Science, Kyushu University International Research Center for Molecular Systems, Kyushu University Center for Advanced Medical Innovation, Kyushu University Department of Biomedical Engineering, Chung Yuan Christian University

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  • Communication to the Editor : Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers

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Abstract

<p>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.</p>

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