Development of integrin targeting liposome for imaging and radionuclide therapy of pancreatic cancer

2014 Fiscal Year Final Research Report

• Project/Area Number: 24591828
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Cancer Center Japan
• Principal Investigator: YOSHIMOTO MITSUYOSHI 独立行政法人国立がん研究センター, その他部局等, 主任研究員 (00345638)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 膵がん / リポソーム / RGD / インテグリン

Outline of Final Research Achievements

αvβ3 integrin is overexpressed in endothelial cells and various tumor cells including pancreatic cancer. In this study, we developed RGD-modified liposomes for imaging and internal radionuclide therapy of pancreatic cancer. We successfully synthesized the RGD-modified liposomes with about 100 nm of particle size. The RGD-modified liposomes dose-dependently inhibited the binding of 125I-echistatin to PANC-1. The IC50 values were 5-67 μM as phospholipids. In contrast, RKG-modified liposome and unmodified liposome did not inhibit the binding. Biodistribution studies using the liposomes loaded with 111In indicated rapid clearance of the RGD-modified liposome from blood. Significant accumulation of radioactivity in spleen was found with increase in the amount of RGD modification (170.4-403.9% ID/g at 24 h). Unmodified liposome showed the highest tumor uptake (2.80% ID/g) at 24 h, whereas the RGD-modified liposomes showed the lower tumor uptake (1.47-2.25% ID/g).

Free Research Field

分子イメージング