title: Controlled synthesis of PEI-coated gold nanoparticles using reductive catechol chemistry for siRNA delivery.
abstract: Development of nano-sized gene delivery vehicles for small interfering RNA (siRNA) delivery is of great importance for their clinical applications such as cancer therapy. Herein, we demonstrate the controlled synthesis of polyethyleneimine (PEI)-coated gold nanoparticles (AuNPs) using catechol-conjugated PEI (PEI-C) for siRNA delivery. Since the conjugated catechol groups are reductive and moderately hydrophobic, PEI-C formed spherical multi-cored micelles in aqueous solution and served as reductive templates for the growth and synthesis of spherical AuNPs with tunable sizes and surface charges. PEI-C was stably anchored on the surface of growing crystal gold seeds with crosslinking, resulting in robust cationic AuNPs. The fabricated PEI-coated AuNPs formed stable complexes with siRNA, and the complexes showed an excellent gene silencing effect in cancer cells. Size and surface charge values of the synthesized AuNPs had a great influence on intracellular uptake and unpacking of siRNA, and the resultant gene silencing efficiency. The PEI-coated AuNPs exhibited an extremely low cytotoxicity due to the reduced density of primary amine groups and the absence of uncomplexed PEI fraction in aqueous solution.
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: Yuhan
authors.initials: Y
authors.lastname: Lee
authors.forename: Soo Hyeon
authors.initials: SH
authors.lastname: Lee
authors.forename: Jee Seon
authors.initials: JS
authors.lastname: Kim
authors.forename: Atsushi
authors.initials: A
authors.lastname: Maruyama
authors.forename: Xuesi
authors.initials: X
authors.lastname: Chen
authors.forename: Tae Gwan
authors.initials: TG
authors.lastname: Park
mesh_terms: D002396:Catechols / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival; D020868:Gene Silencing; D006046:Gold / Q000737:chemistry*; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010084:Oxidation-Reduction; D011094:Polyethyleneimine / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000008:administration & dosage*
chemical_list: D002396:Catechols; D034741:RNA, Small Interfering; D006046:Gold; D011094:Polyethyleneimine; C034221:catechol