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

Haitao Feng; Le Thanh Nam; Takuma Yoshikawa; Akihiro Kishimura; Takeshi Mori; Yoshiki Katayama

doi:10.1248/bpb.b20-00367

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

Haitao Feng, Le Thanh Nam, Takuma Yoshikawa, Akihiro Kishimura, Takeshi Mori, Yoshiki Katayama

Applied Chemistry

Research output: Contribution to journal › Article › peer-review

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>

Original language	English
Pages (from-to)	1301-1305
Number of pages	5
Journal	Biological and Pharmaceutical Bulletin
Volume	43
Issue number	9
DOIs	https://doi.org/10.1248/bpb.b20-00367
Publication status	Published - 2020

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https://doi.org/10.1248/bpb.b20-00367

Cite this

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title = "Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers",

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.",

author = "Haitao Feng and Nam, {Le Thanh} and Takuma Yoshikawa and Akihiro Kishimura and Takeshi Mori and Yoshiki Katayama",

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doi = "10.1248/bpb.b20-00367",

language = "English",

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T1 - Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers

AU - Feng, Haitao

AU - Nam, Le Thanh

AU - Yoshikawa, Takuma

AU - Kishimura, Akihiro

AU - Mori, Takeshi

AU - Katayama, Yoshiki

PY - 2020

Y1 - 2020

N2 - 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.

AB - 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.

U2 - 10.1248/bpb.b20-00367

DO - 10.1248/bpb.b20-00367

M3 - Article

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JO - Biological and Pharmaceutical Bulletin

JF - Biological and Pharmaceutical Bulletin

IS - 9

ER -

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

Abstract

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