Development of tumor-targetable, enzyme-specific activatable fluorescent probe for early diagnosis of tumor

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K07896
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Physical pharmacy
• Research Institution: Hamamatsu University School of Medicine (2016-2017); University of Shizuoka (2015)
• Principal Investigator: Shimizu Kosuke 浜松医科大学, 光尖端医学教育研究センター, 准教授 (30423841)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: がんイメージング / リポソーム / アクチベータブル蛍光プローブ / マクロファージ / DDS / カテプシンB / ホスファチジルセリン

Outline of Final Research Achievements

The aim of this study is to develop a novel near-infrared activatable fluorescent probe which enables to target macrophages in tumor tissues for early diagnosis of tumor. First, I synthesized an activatable fluorescent probe (P-ICG2) which show the near-infrared fluorescent property only after the lysosomal cathepsin B enzymatically cleaves the peptide chain in the probe. On the other hand, to deliver the probe to tumor tissue effectively, I also prepared PS-modified liposomes which can target macrophages infiltrating into tumor tissues. Then, I encapsulated P-ICG2 into the liposomes and developed a macrophage-targetable, enzyme-specific activatable fluorescent probe (P-ICG2-PS-Lip). P-ICG2-PS-Lip showed the fluorescence in lysosomes of mouse macrophage-like RAW264 cells after taking up into the cells. Furthermore, optical imaging of the solid tumor was succeeded, when P-ICG2-PS-Lip was intravenously injected to KLN205 tumor-bearing mouse and the fluorescence imaging was performed.

Free Research Field

薬物送達学