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Di‐ and Triblock siRNA‐PEG Copolymers: PEG Density Effect of Polyelectrolyte Complexes on Cellular Uptake and Gene Silencing Efficiency
Author(s) -
Lee Soo Hyeon,
Mok Hyejung,
Park Tae Gwan
Publication year - 2011
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201000347
Subject(s) - peg ratio , copolymer , pegylation , cationic polymerization , gene silencing , chemistry , conjugate , polymer chemistry , biophysics , ethylene glycol , polymer , biochemistry , polyethylene glycol , organic chemistry , gene , biology , mathematical analysis , mathematics , finance , economics
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.