title: Self-assembled siRNA-PLGA conjugate micelles for gene silencing.
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.
authors.affiliation: Department of Biological Sciences and Graduate School of Nanoscience and Technology, Korea Advanced Institute of Science and Technology, Daejeon 305-701, South Korea.
authors.forename: Soo Hyeon
authors.initials: SH
authors.lastname: Lee
authors.forename: Hyejung
authors.initials: H
authors.lastname: Mok
authors.forename: Yuhan
authors.initials: Y
authors.lastname: Lee
authors.forename: Tae Gwan
authors.initials: TG
authors.lastname: Park
mesh_terms: D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D005260:Female; D020868:Gene Silencing; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008823:Micelles; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D034741:RNA, Small Interfering / Q000737:chemistry*
chemical_list: D008823:Micelles; D034741:RNA, Small Interfering; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid