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 . A block copolymer comprising a hydrophilic polymer segment and a hydrophobic polymer segment,
 wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophilic segment has from 100 to 130 monomer units   wherein 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 n-butyl, 
         wherein n is 1 to about 10, and 
         wherein x is about 20 to about 200 in total. 
       
     
     
         95 . The block copolymer of  claim 94 , wherein the hydrophilic polymer segment comprises PEO. 
     
     
         96 . The block copolymer of  claim 94 , wherein n is 1 to 4. 
     
     
         97 . The block copolymer of  claim 94 , wherein x is about 40 to about 100 in total. 
     
     
         98 .- 103 . (canceled) 
     
     
         104 . The block copolymer of  claim 94 , wherein the block copolymer forms a pH-sensitive micelle. 
     
     
         105 . A composition comprising a pH-sensitive micelle, wherein the pH-sensitive micelle comprises the block copolymer of  claim 94 . 
     
     
         106 . The composition of  claim 105 , wherein the micelle has a size of about 10 to about 200 nm. 
     
     
         107 . The composition of  claim 105 , further comprising a drug encapsulated within the micelle. 
     
     
         108 . The composition of  claim 106 , wherein the drug is a chemotherapeutic agent. 
     
     
         109 . The composition of  claim 107 , wherein the drug is doxorubicin, β-lapachone, or paclitaxel. 
     
     
         110 . A method for treating cancer in an individual in need thereof, comprising administration of an effective amount of the composition of  claim 105 . 
     
     
         111 . The method of  claim 110 , wherein the cancer comprises a solid tumor.