Novel block copolymer and micelle compositions and methods of use thereof

Abstract

wherein R′ is —H or —CH3, wherein R is —NR1R2, wherein R1 and R2 are alkyl groups, wherein R1 and R2 are the same or different, wherein R1 and R2 together have from 5 to 16 carbons, wherein R1 and R2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

1 .- 93 . (canceled) 
     
     
         94 . An in vitro method of imaging a tumor, comprising
 (a) contacting said tumor with a composition comprising a pH sensitive micelle; and   (b) measuring an emission level of a labeling moiety.   
     
     
         95 . The method of  claim 94 , wherein the tumor is of a cancer. 
     
     
         96 . The method of  claim 94 , wherein the tumor is a solid tumor. 
     
     
         97 . The method of  claim 94 , wherein the micelle is dissociated. 
     
     
         98 . The method of  claim 94 , wherein the micelle has a pH transition value. 
     
     
         99 . The method of  claim 98 , wherein the pH transition value is from about 5.9 to about 6.5. 
     
     
         100 . The method of  claim 98 , wherein the pH transition value is from about 5.0 to about 5.5. 
     
     
         101 . The method of  claim 98 , wherein the pH transition value is less than about 1.0 unit. 
     
     
         102 . The method of  claim 98 , wherein the pH transition value less than about 0.5 unit. 
     
     
         103 . The method of  claim 94  wherein the pH sensitive micelle comprising a block copolymer comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises poly(ethylene oxide) (PEO), and the hydrophobic polymer segment comprises 
       
         
           
           
               
               
           
         
         wherein R′ is —H or —CH 3 , 
         wherein R is —NR 1 R 2 , wherein R 1  and R 2  are straight chain alkyl groups, wherein R 1  and R 2  are the same or different, wherein R 1  and R 2  together have from 5 to 16 carbons, wherein R 1  and R 2  may optionally join to form a ring, 
         wherein n is 1 to about 10, 
         wherein x is about 20 to about 200 in total; and 
         wherein the composition comprises a labeling moiety. 
       
     
     
         104 . The method of  claim 103 , wherein the pH sensitive micelle comprises 
       
         
           
           
               
               
           
         
         wherein R′″ is a suitable moiety that is resulting from a polymerization reaction; 
         wherein L is a labeling moiety; 
         wherein x is about 20 to about 200; and 
         wherein y is about 1 to about 6. 
       
     
     
         105 . The method of  claim 104 , wherein L is a fluorescent label or a near infrared label.