Jeong Ji Hoon, Kim Sung Wan, Park Tae Gwan
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305-701, South Korea.
J Control Release. 2003 Dec 5;93(2):183-91. doi: 10.1016/j.jconrel.2003.07.002.
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.
合成了反义c-raf寡核苷酸（ODN）与聚乙二醇（PEG）的缀合物用于细胞内ODN递送。当与聚乙烯亚胺（PEI）结合时，ODN-PEG缀合物在水溶液中自缔合形成聚电解质复合胶束。胶束的有效流体动力学直径约为70 nm，粒径分布窄。流式细胞术分析表明，A2780细胞对胶束的细胞摄取远高于单独的ODN。该胶束在体外和体内对卵巢癌细胞也显示出优异的抗增殖活性。
