BLOCK COPOLYMERS FOR STABLE MICELLES
The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same. Compositions herein are useful for drug-delivery applications.
1 . A triblock copolymer of formula II:
wherein:
n is 20-500;
m is 0, 1, or 2;
x is 3 to 50;
y is 5 to 100;
R y is selected from one or more natural or unnatural amino acid side chain groups such that the overall block is hydrophobic;
R 1 is —Z(CH 2 CH 2 Y) p (CH 2 ) t R 3 , wherein:
Z is —O—, —NH—, —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 hydrogen, —N 3 , —CN, —NH 2 , —CH 3 ,
a strained cyclooctyne moiety, a mono-protected amine, a di-protected amine, an optionally protected aldehyde, an optionally protected hydroxyl, an optionally protected carboxylic acid, an optionally protected thiol, 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.
2 . A triblock copolymer of claim 1 wherein the structure is:
3 . A triblock copolymer of claim 1 wherein R 3 is
4 . A triblock copolymer of claim 1 wherein R 3 is —CH 3 .
5 . A triblock copolymer of claim 1 wherein m is 2.
6 . A triblock copolymer of claim 1 wherein R y is a mixture of leucine and tyrosine side chain groups.
7 . A triblock copolymer of claim 1 wherein R y is a mixture of phenylalanine and tyrosine side chain groups.
8 . A triblock copolymer of claim 1 wherein R y is a mixture of leucine, aspartic acid, and tyrosine side chain groups.
9 . A triblock copolymer of claim 1 wherein R y is a mixture of phenylalanine, aspartic acid, and tyrosine side chain groups.