AMPHIPHILIC NANOPARTICLES FOR CODELIVERY OF WATER-INSOLUBLE SMALL MOLECULES AND RNAi

A composition comprising:

• an optional pharmaceutically acceptable carrier;
• an siRNA;
• an anticancer agent;
• and
• a block copolymer comprising:
• (i) a first block comprising a plurality of first monomers, wherein each first monomer is selected from the group consisting of ethylene glycol, propylene glycol, vinyl alcohol, acrylic acid, methacrylic acid, methyl acrylate, methyl methacrylate, ethyl acrylate, ethyl methacrylate, hydroxyethyl methacrylate, 2,3-dihydroxypropyl methacrylate, vinyl pyrrolidone, and dextrin;
• (ii) a second block comprising a plurality of second monomers, wherein each second monomer is selected from the group consisting of 6-hydroxycaproic acid, side-chain N-protected lysine, lactic acid, glycolic acid, hydroxybutyrate, valine, isoleucine, leucine, methionine, phenylalanine, tryptophan, cysteine, alanine, proline, glycine, tyrosine, side-chain carbonyl-protected aspartic acid, side-chain carbonyl-protected glutamic acid, propylene carbonate, butyl acrylate, butyl methacrylate, and benzyl methacrylate;
• and
• (iii) a third block comprising a plurality of third monomers, wherein each third monomer is selected from the group consisting of lysine, side-chain aminoalkyl-functionalized lysine, asparagine, side-chain aminoalkyl-functionalized asparagine, arginine, aspartamide, side-chain aminoalkyl-functionalized aspartamide, and ethyleneimine,
• wherein
• the siRNA is non-covalently associated with the block copolymer;
• and
• the anticancer agent is associated with the block copolymer.