A new antisense oligonucleotide delivery system based on self-assembled ODN-PEG hybrid conjugate micelles. |
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Authors: | Ji Hoon Jeong Sung Wan Kim Tae Gwan Park |
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Institution: | Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305-701, South Korea. |
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Abstract: | The conjugate of antisense c-raf oligonucleotide (ODN) and poly(ethylene glycol) (PEG) was synthesized for intracellular ODN delivery. When combined with polyethylenimine (PEI), the ODN-PEG conjugate self-associated to form polyelectrolyte complex micelles in aqueous solution. The effective hydrodynamic diameter of the micelles was ca. 70 nm with a narrow size distribution. Flow cytometry analysis indicated that the cellular uptake of the micelles by A2780 cells was much higher than that of ODN alone. The micelles also showed a superior antiproliferative activity against ovarian cancer cells in vitro and in vivo. |
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