Abstract
A new siRNA delivery system using a cationic glyco-star polymer is described. Spermine-modified 8-arm amylose star polymer (with a degree of polymerization of approximately 60 per arm) was synthesized by chemoenzymatic methods. The cationic star polymer effectively bound to siRNA and formed spherical complexes with an average hydrodynamic diameter of 230 nm. The cationic 8-arm star polymer complexes showed superior cellular uptake characteristics and higher gene silencing effects than a cationic 1-arm polymer. These results suggest that amylose-based star polymers are a promising nanoplatform for glycobiomaterials.
Highlights
Since the discovery of RNA interference (RNAi) [1] and the achievement of gene silencing by synthetic small interfering RNAs [2], siRNA has become established as a new tool for silencing target genes. siRNAs have, been widely recognized as novel potential therapeutics
We report that a spermine-modified amylose-based star polymer acts as a siRNA carrier. siRNApolymer complexes were characterized with respect to their sizes and charge ratios
We have demonstrated the utility of cationic glyco-star polymers as carriers for siRNA delivery
Summary
Since the discovery of RNA interference (RNAi) [1] and the achievement of gene silencing by synthetic small interfering RNAs (siRNAs) [2], siRNA has become established as a new tool for silencing target genes. siRNAs have, been widely recognized as novel potential therapeutics. Since the discovery of RNA interference (RNAi) [1] and the achievement of gene silencing by synthetic small interfering RNAs (siRNAs) [2], siRNA has become established as a new tool for silencing target genes. SiRNAs have, been widely recognized as novel potential therapeutics. There has been considerable effort to develop siRNA therapeutics for treating viral infections and cancers [3]. For siRNA therapeutic applications, appropriate gene carriers are required because naked siRNA is readily degraded by nucleases. SiRNAs are too large and hydrophilic to cross cell membranes without a delivery method [4, 5]. To successfully deliver siRNAs, the carriers must penetrate biological barriers. The development of gene carriers to efficiently deliver siRNAs remains an important challenge
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