Self-assembled siRNA-PLGA conjugate micelles for gene silencing

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

doi:10.1016/j.jconrel.2010.12.007

Self-assembled siRNA-PLGA conjugate micelles for gene silencing

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

Research output: Contribution to journal › Article › peer-review

91 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 language	English
Pages (from-to)	152-158
Number of pages	7
Journal	Journal of Controlled Release
Volume	152
Issue number	1
DOIs	https://doi.org/10.1016/j.jconrel.2010.12.007
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

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10.1016/j.jconrel.2010.12.007

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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 \textasciitilde{} 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 \textasciitilde{} 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.",

keywords = "Linear polyethylenimine, PLGA, Self-assembled micelles, Target gene silencing, siRNA",

author = "Lee, \{Soo Hyeon\} and Hyejung Mok and Yuhan Lee and Park, \{Tae Gwan\}",

year = "2011",

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day = "30",

doi = "10.1016/j.jconrel.2010.12.007",

language = "English",

volume = "152",

pages = "152--158",

journal = "Journal of Controlled Release",

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T1 - Self-assembled siRNA-PLGA conjugate micelles for gene silencing

AU - Lee, Soo Hyeon

AU - Mok, Hyejung

AU - Lee, Yuhan

AU - Park, Tae Gwan

PY - 2011/5/30

Y1 - 2011/5/30

N2 - 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.

AB - 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.

KW - Linear polyethylenimine

KW - PLGA

KW - Self-assembled micelles

KW - Target gene silencing

KW - siRNA

UR - https://www.scopus.com/pages/publications/79958168461

U2 - 10.1016/j.jconrel.2010.12.007

DO - 10.1016/j.jconrel.2010.12.007

M3 - Article

C2 - 21185893

AN - SCOPUS:79958168461

SN - 0168-3659

VL - 152

SP - 152

EP - 158

JO - Journal of Controlled Release

JF - Journal of Controlled Release

IS - 1

ER -

Self-assembled siRNA-PLGA conjugate micelles for gene silencing

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Keywords

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