Synthesis of siRNA Polyplexes Adopting a Combination of RAFT Polymerization and Thiol-ene Chemistry

被引:36
作者
Valade, David [1 ,2 ]
Boyer, Cyrille [1 ]
Davis, Thomas P. [1 ]
Bulmus, Volga [2 ]
机构
[1] Univ New S Wales, Sch Chem Sci & Engn, CAMD, Sydney, NSW 2052, Australia
[2] Univ New S Wales, Sch Biotechnol & Biomol Sci BABS, Sydney, NSW 2052, Australia
基金
澳大利亚研究理事会;
关键词
CROSS-LINKED MICELLES; BLOCK-COPOLYMERS; RADICAL POLYMERIZATION; ALLYL METHACRYLATE; DELIVERY-SYSTEMS; RNA INTERFERENCE; GENE DELIVERY; POLYMERS; CHAIN; FUNCTIONALIZATION;
D O I
10.1071/CH09208
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Block copolymers of allyl methacrylate and N-(2-hydroxypropyl) methacrylamide (HPMA) with different block lengths have been synthesized by reversible addition-fragmentation chain transfer polymerization. Allyl groups were modified with cysteamine, via a thiol-ene photoreaction, with a high efficiency (similar to 100%)as evidenced by NMR spectroscopy, yielding cationic copolymers of HPMA. Polyelectrolyte complexes of small interfering RNAs (siRNA) and the cationic block copolymers were then formed at an N/P ratio between 1 and 4 depending on the block length of the copolymers. Increasing the length of the hydrophilic block was found to decrease the efficiency of siRNA complexation. The hydrodynamic diameter of the polyplexes in 130 mM buffer solution was less than 100 nm.
引用
收藏
页码:1344 / 1350
页数:7
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