Abstract
Biodegradable poly(D,L-lactic-co-glycolic acid) (PLGA) was conjugated to the 3′ end of small interfering RNA (siRNA) via a disulfide bond to synthesize siRNA-PLGA hybrid conjugates. siRNA-PLGA conjugates were spontaneously self-assembled to form a spherical core/shell type micellar structure of ~ 20 nm in an aqueous environment, probably by hydrophobic interaction of PLGA blocks in the core surrounded by an siRNA shell layer. When linear polyethylenimine was added to the siRNA-PLGA micelles in aqueous solution, stable siRNA-PLGA/LPEI micelles with a size of ~ 30 nm were produced via ionic complexation between siRNA and LPEI in the outer shell. The cationic siRNA-PLGA/LPEI micelles showed superior intracellular uptake and enhanced gene silencing effect, compared to naked siRNA/LPEI complexes. The hybrid micelle structure based on siRNA and PLGA can be potentially used as an efficient siRNA delivery system for gene silencing.
Original language | English |
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Pages (from-to) | 152-158 |
Number of pages | 7 |
Journal | Journal of Controlled Release |
Volume | 152 |
Issue number | 1 |
DOIs | |
State | Published - May 30 2011 |
Externally published | Yes |
Funding
This study was supported by the Intelligent Drug Delivery System grant and World Class University program from the Ministry of Education, Science and Technology, Republic of Korea .
Keywords
- Linear polyethylenimine
- PLGA
- Self-assembled micelles
- Target gene silencing
- siRNA