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Oligonucleotide core carrier compositions for delivery of nucleic acid-containing therapeutic agents, methods of making and using the same

  • US 8,563,527 B2
  • Filed: 08/19/2008
  • Issued: 10/22/2013
  • Est. Priority Date: 08/20/2007
  • Status: Active Grant
First Claim
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1. An oligonucleotide-core carrier composition comprising:

  • (i) a carrier;

    (ii) at least one of a first single stranded oligonucleotide group covalently linked to the carrier, wherein the oligonucleotide group is less than 100 bases;

    (iii) a plurality of polymeric protective side chains, wherein each protective side chain is covalently linked and pendant to the carrier and/or to the first oligonucleotide group wherein each protective side chain has a molecular weight between about 400 and 20,000 Daltons independent of the carrier weight and the first oligonucleotide group weight; and

    (iv) a load molecule, wherein the load molecule comprises a peptide/protein covalently bonded to a second single stranded oligonucleotide group with an essentially complementary sequence to the first single stranded oligonucleotide group and dissociably linked by nucleotide hydrogen bonding base pairing to the first oligonucleotide group;

    wherein said carrier is a polymer selected from the group consisting of a polyamino acid, a polyethyleneimine, a polyallyamine, a chitosan, a polysaccharide, an oligosaccharide, a natural saccharide, an aminated and carboxylated polysaccharide, an aminated and carboxylated oligosaccharide, a sulfonated polysaccharide, a sulfonated oligosaccharide, an aminocarboxylated polysaccharide, an aminocarboxylated oligosaccharide, a carboxymethylated polysaccharide, a carboxymethylated oligosaccharide, a polyamidoamine, a polyacrylic acid, a polyvinyl alcohol, and a polythiol; and

    further wherein the plurality of polymeric protective side chains comprises polyethylene glycol, polypropylene glycol, or a co-polymer of polyethylene glycol and polypropylene glycol.

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