| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2014: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Outline of Final Research Achievements |
The installation of ligand molecules such as peptides onto nanocarriers is now considered an important strategy to improve the selectivity of drug delivery. Among these ligands, Arg-Gly-Asp (RGD) peptides are promising ligand molecules for targeting alpha v beta 3 integrins, which are overexpressed in angiogenic sites and tumors, such as human glioblastoma (U87MG). In this study, the cyclic RGD was introduced to the maleimide-surface functionalized dichloro(1,2-diamino-cyclohexane)platinum(II)-loaded micelles by Michael addition reaction. Intravital confocal laser scanning microscopy revealed that the cRGD-linked polymeric micelles (cRGD/m) accumulated rapidly and had high permeability from vessels into the tumor parenchyma. It was confirmed that the selective and accelerated accumulation of cRGD/m into tumors occurred via an active internalization pathway, possibly transcytosis, thereby producing significant anti-tumor effects in an orthotopic mouse model of U87MG human glioblastoma.
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