LHRH Receptor-Mediated Delivery of siRNA Using Polyelectrolyte Complex Micelles Self-Assembled from siRNA-PEG-LHRH Conjugate and PEI

被引：90

作者：

Kim, Sun Hwa ^{[1
,2
]}

Jeong, Ji Hoon ^{[3
]}

Lee, Soo Hyeon ^{[1
]}

Kim, Sung Wan ^{[2
]}

Park, Tae Gwan ^{[1
]}

机构：

[1] Korea Adv Inst Sci & Technol, Dept Biol Sci, Taejon 305701, South Korea

[2] Univ Utah, Dept Pharmaceut & Pharmaceut Chem, Ctr Controlled Chem Delivery, Salt Lake City, UT 84112 USA

[3] Sungkyunkwan Univ, Coll Pharm, Suwon 440746, South Korea

来源：

BIOCONJUGATE CHEMISTRY | 2008年 / 19卷 / 11期

关键词：

D O I：

10.1021/bc800249n

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Polyelectrolyte complex (PEC) micelles modified with cancer cell targeting moieties were prepared for intracellular delivery of vascular endothelial growth factor (VEGF) small interfering RNA (siRNA). A luteinizing hormone-releasing hormone (LHRH) peptide analogue was coupled as a cancer targeting ligand to the distal end of the poly(ethylene glycol) (PEG)-siRNA conjugate. The siRNA-PEG-LHRH conjugate self-assembled to form nanosized PEC micelles upon mixing with poly(ethylenimine) (PEI) via ionic interactions. The PEC micelles showed spherical morphology with a hydrodynamic diameter of ca. 150 nm. For LHRH receptor overexpressing ovarian cancer cells (A2780), the PEC micelles with LHRH exhibited enhanced cellular uptake compared to those without LHRH, resulting in increased VEGF gene silencing efficiency via receptor-mediated endocytosis. This study showed that PEC micelles decorated with specific cell-recognizable targeting ligands could be used for targeted delivery of siRNA.

引用

页码：2156 / 2162

页数：7

共 24 条

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