Patent ID: 8299128

Claim:
A composition comprising a drug-loaded micelle and a pharmaceutically acceptable carrier, adjuvant, or vehicle, wherein the micelle comprises a multiblock copolymer, wherein said micelle has a drug-loaded inner core, a non-crosslinked outer core, and a hydrophilic shell, wherein the multiblock copolymer is of formula I: wherein: n is 10-2500; m is 1 to 1000; m′ is 1 to 1000; R x is a natural or unnatural amino acid side-chain group that is capable of crosslinking; R y is a hydrophobic or ionic, natural or unnatural amino acid side-chain group; R 1 is —Z(CH 2 CH 2 Y) p (CH 2 ) t R 3 , wherein: Z is —O—, —S—, —C≡C—, or —CH 2 —; each Y is independently —O— or —S—; p is 0-10; t is 0-10; and R 3 is —N 3 , —CN, a mono-protected amine, a di-protected amine, a protected aldehyde, a protected hydroxyl, a protected carboxylic acid, a protected thiol, a 9-30 membered crown ether, or an optionally substituted group selected from aliphatic, a 5-8 membered saturated, partially unsaturated, or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, an 8-10 membered saturated, partially unsaturated, or aryl bicyclic ring having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a detectable moiety; Q is a valence bond or a bivalent, saturated or unsaturated, straight or branched C 1-12 alkylene chain, wherein 0-6 methylene units of Q are independently replaced by -Cy-, —O—, —NH—, —S—, —OC(O)—, —C(O)O—, —C(O)—, —SO—, —SO 2 —, —NHSO 2 —, —SO 2 NH—, —NHC(O)—, —C(O)NH—, —OC(O)NH—, or —NHC(O)O—, wherein: -Cy- is an optionally substituted 5-8 membered bivalent, saturated, partially unsaturated, or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an optionally substituted 8-10 membered bivalent saturated, partially unsaturated, or aryl bicyclic ring having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R 2a is a mono-protected amine, a di-protected amine, —N(R 4 ) 2 , —NR 4 C(O)R 4 , —NR 4 C(O)N(R 4 ) 2 , —NR 4 C(O)OR 4 , or —NR 4 SO 2 R 4 ; and each R 4 is independently an optionally substituted group selected from hydrogen, aliphatic, a 5-8 membered saturated, partially unsaturated, or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, an 8-10 membered saturated, partially unsaturated, or aryl bicyclic ring having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a detectable moiety, or: two R 4 on the same nitrogen atom are taken together with said nitrogen atom to form an optionally substituted 4-7 membered saturated, partially unsaturated, or aryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur.