| 研究実績の概要 |
The purpose of the current research is to construct PIC micelles, where, a widely used amimoglycoside antibiotic Neomycin, that has specific RNA-binding ability and also has anti-angiogenin property, will be used as polycationic segments to hold polyanionic siRNA or other nucleic acid type biomolecules for combination-therapy against cancer. In terms of polymer synthesis, we have prepared two novel block copolymers conjugated with azide functionalized neomycin through Huisgen 1,3-Dipolar Cycloaddition between the azide function of neomycin and alkyne function of polymer. Alkyne functional group was introduced in poly(ethylene glycol)-b-poly(β-benzyl-aspartamide) polymers via aminolysis reaction utilizing an amine and alkyne containing bi-functional linker. In one polymer, we used single arm polyethylene glycol (PEG) having molecular weight of 12Kilo Dalton (KD) and with 20 repeating units of poly amino acid segments; this polymer and nucleic acid complex, self assembled in a PIC micelle type structure. In another polymer we utilized dual armed PEG with each arm having molecular weight of 40 KD and with only 6 repeating units of poly amino acid segments, this polymer was prepared to form Unit PIC type particles with a single polymer and single siRNA.
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