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SYNTHESIS OF BIODEGRADABLE CATIONIC TRIBLOCK COPOLYMER mPEG-PCL-PLL FOR siRNA DELIVERY

机译:用于siRNA递送的可生物降解阳离子三嵌段共聚物MPEG-PCL-PLL的合成

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Amino-terminated methoxy poly(ethylene glycol)-b-poly(e-caprolactone) (mPEG-PCL-NH2) was synthesized by azidizing the end OH group of mPEG-PCL and by subsequent hydrogenation of the azido group. It was used to initiate ring-opening polymerization of ε-CBz (L-lysine)-N-carboxyanhydride to obtain cationic triblock copolymer methoxy poly(ethylene glycol)-b-poly(ε-caprolactone)-b-poly(L-lysine) (mPEG-PCL-PLL). The copolymer could self-assemble directly in water into nanoscale micelles with a hydrophobic core and a cationic corona. Therefore, they can further complex with anionic siRNA for possible application in gene delivery.
机译:通过氧化聚氯乙烯基团的末端OH基团并随后的氮杂基氢化来合成氨基封端的甲氧基聚(乙二醇)-B-聚(E-己内酯)(MPEG-PCL-NH2)。它用于引发ε-CBZ(L-赖氨酸)-N-羧酐的开环聚合,得到阳离子三嵌段共聚物甲氧基聚(乙二醇)-B-聚(ε-己内酯)-B-聚(L-赖氨酸)(MPEG-PCL-PLL)。共聚物可以用疏水芯和阳离子电晕将水中直接自组装成纳米级胶束。因此,它们可以进一步复杂于阴离子siRNA,以便在基因递送中施用。

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