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Peptide‐like Polymers Exerting Effective Glioma‐Targeted siRNA Delivery and Release for Therapeutic Application
Author(s) -
An Sai,
He Dongsheng,
Wagner Ernst,
Jiang Chen
Publication year - 2015
Publication title -
small
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.785
H-Index - 236
eISSN - 1613-6829
pISSN - 1613-6810
DOI - 10.1002/smll.201501167
Subject(s) - glioma , small interfering rna , gene silencing , rna interference , peptide , cytotoxicity , chemistry , transfection , intracellular , ethylene glycol , biophysics , cancer research , biochemistry , in vitro , rna , biology , gene , organic chemistry
Lipopolymer 49, a solid‐phase synthesized T‐shaped peptide‐like oligoamide containing two central oleic acids, 20 aminoethane, and two terminal cysteine units, is identified as very potent and biocompatible small interfering RNA (siRNA) carrier for gene silencing in glioma cells. This carrier is combined with a novel targeting polymer 727, containing a precise sequence of Angiopep 2 targeting peptide, linked with 28 monomer units of ethylene glycol, 40 aminoethane, and two terminal cysteines in siRNA complex formation. Angiopep‐polyethylene glycol (PEG)/siRNA polyplexes exhibit good nanoparticle features, effective glioma‐targeting siRNA delivery, and intracellular siRNA release, resulting in an outstanding gene downregulation both in glioma cells and upon intravenous delivery in glioma model nude mice without significant biotoxicity. Therefore, this novel siRNA delivery system is expected to be a promising strategy for targeted and safe glioma therapy.