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Polyspermine Imidazole-4,5-imine, a Chemically Dynamic and Biologically Responsive Carrier System for Intracellular Delivery of siRNA

Authors

  • Shiyue Duan,

    1. Laboratory of Drug Delivery and Biomaterials, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240 (P.R. China)
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  • Weien Yuan,

    1. Laboratory of Drug Delivery and Biomaterials, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240 (P.R. China)
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  • Fei Wu,

    1. Laboratory of Drug Delivery and Biomaterials, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240 (P.R. China)
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  • Tuo Jin

    Corresponding author
    1. Laboratory of Drug Delivery and Biomaterials, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240 (P.R. China)
    • Laboratory of Drug Delivery and Biomaterials, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240 (P.R. China)
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  • We thank the Ministry of Science and Technology (2009ZX09310-007) of the People’s Republic of China and the Technology Committee of Science and Technology Special Nanotechnology Grant (No. 1052nm03900) for financial support. We also acknowledge Prof. Y. H. Xu (School of Pharmacy, Shanghai Jiao Tong University) for providing SMMC-7721 cells stably expressing the pGL3 luciferase gene.

Abstract

original image

Silence please! Polyspermine imidazole-4,5-imine (blue lines) was formed by condensing spermine with bisformaldehyde imidazole through a pH-responsive linkage. This polymer was used to condense siRNAs into nanoparticles (see scheme) and studied for delivery into cells and release from endosomes. Cellular and in vivo assays indicated that this siRNA carrier was efficient in silencing target genes with negligible cytotoxicity.

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