Department of Biological Sciences and Graduate School of Nanoscience and Technology, Korea Advanced Institute of Science and Technology, Daejeon, South Korea.
Macromol Biosci. 2011 Mar 10;11(3):410-8. doi: 10.1002/mabi.201000347. Epub 2010 Nov 15.
Di- and triblock siRNA/PEG copolymers were synthesized and complexed with cationic SLN for assessing their gene silencing efficiency as a function of PEG density. A sssiRNA and a sassiRNA were separately conjugated with PEG via a disulfide linkage. AB-type diblock and ABA-type triblock copolymers were successfully prepared by stoichiometric hybridization of sssiRNA-PEG conjugate with sassiRNA and sassiRNA-PEG conjugate, respectively. The resultant di- and triblock copolymers were characterized by means of GPC and gel electrophoresis. The serum stability of siRNA in the copolymers was enhanced as compared to that of naked siRNA. Using cationic SLN as a model carrier, the PEGylation density effect of the siRNA-PEG/SLN complexes on gene silencing and cellular uptake was analyzed.
二嵌段和三嵌段 siRNA/PEG 共聚物被合成并与阳离子 SLN 复合，以评估其作为 PEG 密度函数的基因沉默效率。sssiRNA 和 sssiRNA 分别通过二硫键与 PEG 连接。AB 型二嵌段和 ABA 型三嵌段共聚物通过 sssiRNA-PEG 缀合物与 sassiRNA 和 sassiRNA-PEG 缀合物的化学计量杂交成功制备。所得的二嵌段和三嵌段共聚物通过 GPC 和凝胶电泳进行了表征。与裸 siRNA 相比，共聚物中 siRNA 的血清稳定性得到了增强。使用阳离子 SLN 作为模型载体，分析了 siRNA-PEG/SLN 复合物的 PEG 化密度对基因沉默和细胞摄取的影响。
