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Title: PH-labile sheddable block copolymers by RAFT polymerization: Synthesis and potential use as siRNA conjugates
Authors: Huang, Xin
Sevimli, Sema İlknur
Bulmuş, Volga
Keywords: Bioconjugate
Block copolymer
Drug delivery
RAFT polymerization
siRNA delivery
Polyethylene glycols
Issue Date: Oct-2013
Publisher: Elsevier Ltd.
Source: Huang, X., Sevimli, S. İ., and Bulmuş, V. (2013). PH-labile sheddable block copolymers by RAFT polymerization: Synthesis and potential use as siRNA conjugates. European Polymer Journal, 49(10), 2895-2905. doi:10.1016/j.eurpolymj.2013.03.036
Abstract: Well-defined amphiphilic block copolymers composed of hydrophilic and hydrophobic blocks linked through an acid-labile acetal bond were synthesized directly by RAFT polymerization using a new poly(ethylene glycol) (PEG) macroRAFT agent modified with an acid-labile group at its R-terminal. The new macroRAFT agent was used for polymerization of poly(t-butyl methacrylate) (PtBMA) or poly(cholesterol-methacrylate) (PCMA) to synthesize well-defined block copolymers with a PEG block sheddable under acidic conditions. The chain extension polymerization kinetics showed known traits of RAFT polymerization. The molecular weight distributions of the copolymers prepared using the new macroRAFT agent remained below 1.2 during the polymerizations and the molecular weight of the copolymers was linearly proportional to monomer conversions. The acid-catalyzed hydrolysis behavior of the PEG-macroRAFT agent and the PEG-b-PtBMA (Mn = 13,600 by GPC, PDI = 1.10) was studied by GPC, 1H NMR and UV-vis spectroscopy. The half-life of acid-hydrolysis was 70 min at pH 2.2 and 92 h at pH 4.0. The potential use of the pH-labile shedding behavior of the copolymers was demonstrated by conjugating a thiol-modified siRNA to ω-pyridyldisulfide modified PEG-b-PCMA. The resultant PEG-b-PCMA-b-siRNA triblock modular polymer released PCMA-b-siRNA segment in acidic and siRNA segment in reductive conditions, as confirmed by polyacrylamide gel electrophoresis.
ISSN: 0014-3057
Appears in Collections:Chemical Engineering / Kimya Mühendisliği
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

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