Journal
ADVANCED FUNCTIONAL MATERIALS
Volume 28, Issue 6, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adfm.201703207
Keywords
antitumor treatment; functionalization by surface assembly; siRNA delivery; unimolecular polyplexes; Zeta potential regulated polymerization
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Funding
- Natural Science Foundation of China [81373352, 81690262]
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A synthetic carrier of small interfering RNA (siRNA) with customizable size, pH-responsive degradability and optimized surface population of cell-targeting agents is constructed precisely through a series of interlocked thermodynamically self-regulated processes. This system consists of a unimolecular polyplex core formed from each individual molecule of networked cationic polymer and a multi-functional shell assembled from a rationally designed triblock copolymer. The core-forming polymer of defined size is synthesized via Zeta potential-regulated condensation of branched and linear multi-amine bearing oligomers through pH-responding imidazole conjugated imine linkages. The shell-forming copolymer consists of a multi-carboxyl saccharide end block to guide to the surface assembly, a hydrophobic central block to form an encapsulating layer, and a poly(ethylene glycol) end block equipped with a highly selective active ester for hooking various cell-targeting agents. Animal assays confirm the flexibility and convenience of this system to equip with selected functional components for systemic delivery of siRNA.
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