SELF-ASSEMBLED PARTICLES FROM ZWITTERIONIC POLYMERS AND RELATED METHODS

摘要

Zwitterionic block copolymers and zwitterionic conjugates that advantageously self-assemble into particles, particles assembled from the zwitterionic block copolymers and zwitterionic conjugates, pharmaceutical compositions that include the self-assembled particles, and methods for delivering therapeutic and diagnostic agents using the particles.

主权项

1. A block copolymer, comprising:
(a) a zwitterionic polymer block comprising a poly(carboxybetaine); and (b) a hydrophobic block, wherein the zwitterionic polymer block comprises a plurality of repeating units, each repeating unit having the formula: wherein R1 is selected from the group consisting of hydrogen, fluorine, trifluoromethyl, C1-C6 alkyl, and C6-C12 aryl groups; R2 and R3 are independently selected from the group consisting of alkyl and aryl, or taken together with the nitrogen to which they are attached form a cationic center; L1 is a linker that covalently couples the cationic center [N+(R5)(R6)] to the polymer backbone [—(CH2—CR4)n—]; L2 is a linker that covalently couples the anionic center [A(═O)—O−] to the cationic center; A is C; M+ is a counter ion associated with the (A=O)O− anionic center; X− is a counter ion associated with the cationic center; and n is an integer from 1 to about 10,000.