Abstract

We have recently and successfully developed DNA quadruplex hydrogel, which instantly turn into gel in response to K + or Na + addition, by directly coupling several deoxyguanosine residues to the both ends of polyethylene glycols utilizing High-Efficiency Liquid-Phase (HELP) large-scale DNA synthesis technique. In this study, we examined a utility of this hydrogel as a Drug Delivery System (DDS) carrier. We found that nanoparticles of 100–200 nm diameter can be efficiently prepared by forming gels in sufficiently diluted solution of the macromonomers. The nanogels were fully characterized by dynamic light scattering (DLS) and atomic force microscopy (AFM). High-speed video-rate AFM measurements enabled direct and real-time observation of selective dissolution of DNA Quadruplex nanogels triggered by the addition of a crown ether into the system. Drug loading of G-quaduplex-binding anticancer drug and its delivery into cells were also accomplished.

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