Synthesis of Statistical Copolymers Containing Multiple Functional Peptides for Nucleic Acid Delivery

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• 作者：Russell N. Johnson ; Rob S. Burke ; Anthony J. Convertine ; Allan S. Hoffman ; Patrick S. Stayton ; Suzie H. Pun
• 刊名：Biomacromolecules
• 出版年：2010
• 出版时间：November 8, 2010
• 年：2010
• 卷：11
• 期：11
• 页码：3007-3013
• 全文大小：322K
• 年卷期：v.11,no.11(November 8, 2010)
• ISSN：1526-4602

文摘

Our report describes RAFT copolymerization of multiple species of active peptide monomers with N-(2-hydroxypropyl(methacrylamide) (HPMA) under aqueous conditions. Resulting statistical copolymers are narrowly disperse with highly controlled molecular weight and composition. Side-chain peptide copolymers were synthesized using a DNA condensing peptide (K<sub>12sub>), and an endosomal escape peptide (K<sub>6sub>H<sub>5sub>) that had been modified with an aminohexanoic linker and capped with methacrylamide vinyl on the NH<sub>2sub>-terminus. Copolymers of HMPA-co-K<sub>12sub> and HPMA-co-K<sub>12sub>-co-K<sub>6sub>H<sub>5sub> efficiently condensed DNA into small particles that maintain size stability even in 150 mM salt solutions. With increasing peptide content, the peptide-based polymers demonstrated gene delivery efficiencies to HeLa cells that were comparable to branched polyethylenimine.