Self-assembled siRNA-PLGA conjugate micelles for gene silencing

Soo Hyeon Lee, Hyejung Mok, Yuhan Lee, Tae Gwan Park

Research output: Contribution to journalArticlepeer-review

87 Scopus citations

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 languageEnglish
Pages (from-to)152-158
Number of pages7
JournalJournal of Controlled Release
Volume152
Issue number1
DOIs
StatePublished - May 30 2011
Externally publishedYes

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

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