NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

1 . 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 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 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 block copolymer optionally comprises a labeling moiety.

2 . (canceled)

3 . The block copolymer of claim 1 , wherein n is 1 to 4.

4 . (canceled)

5 . The block copolymer of claim 1 , wherein R′ is —CH 3 .

6 . The block copolymer of claim 1 , wherein R′ is —H.

7 . The block copolymer of claim 1 , wherein x is about 40 to about 100 in total.

8 .- 11 . (canceled)

12 . The block copolymer of claim 1 , wherein R 1 and R 2 are each straight or branched alkyl.

13 . The block copolymer of claim 1 , wherein R 1 and R 2 join to form a ring.

14 . The block copolymer of claim 1 , wherein R 1 and R 2 are the same.

15 . The block copolymer of claim 1 , wherein R 1 and R 2 are different.

16 . The block copolymer of claim 1 , wherein R 1 and R 2 each have 3 to 8 carbons.

17 . The block copolymer of claim 13 , wherein R 1 and R 2 together form a ring having 5 to 10 carbons.

18 . The block copolymer of claim 1 , wherein R 1 and R 2 are propyl or butyl.

19 . (canceled)

20 . The block copolymer of claim 1 , wherein R 1 and R 2 are butyl.

21 . (canceled)

22 . The block copolymer of claim 1 , wherein R 1 and R 2 together are —(CH 2 ) 5 —.

23 . The block copolymer of claim 1 , wherein R 1 and R 2 together are —(CH 2 ) 6 —.

24 . The block copolymer of claim 1 , comprising a compound of Formula I:

wherein L is a labeling moiety,

wherein y is 0 to about 6,

wherein R″ is —H or —CH 3 ;

wherein m is 1 to about 10;

wherein z is such that the PEO is about 2 kD to about 20 kD in size,

wherein R′″ is any suitable moiety, and

wherein the following portion of the structure:

may be arranged in any order.

25 . The block copolymer of claim 24 , wherein R″ is —CH 3 .

26 . The block copolymer of claim 24 , wherein R″ is —H.

27 . The block copolymer of claim 24 , wherein m is 1 to 4.

28 . (canceled)

29 . The block copolymer of claim 24 , wherein the PEO is about 2 kD to about 10 kD in size.

30 . The block copolymer of claim 24 , wherein the PEO is about 4 kD to about 6 kD in size.

31 . The block copolymer of claim 24 , wherein the PEO is about 5 kD in size.

32 . The block copolymer of claim 28 , wherein z is about 114.

33 . The block copolymer of claim 24 , wherein y is 0.

34 . The block copolymer of claim 24 , wherein y is 1 to 6.

35 . (canceled)

36 . The block copolymer of claim 24 , wherein L is a fluorescent label.

37 . (canceled)

38 . The block copolymer of claim 24 , wherein L is a near-infrared (NIR) label.

39 . The block copolymer of claim 38 , wherein the NIR label is cypate or a cypate analog.

40 .- 41 . (canceled)

42 . A composition comprising a pH-sensitive micelle, wherein the pH-sensitive micelle comprises 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 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 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 block copolymer optionally comprises a labeling moiety.

43 .- 70 . (canceled)

71 . A method for treating cancer in an individual in need thereof, comprising administration of an effective amount of a composition of of claim 42 , wherein said pH sensitive micelle encapsulates a chemotherapeutic drug.

72 . (canceled)

73 . A method for imaging a tumor in an individual, comprising

a) administering a composition of claim 42 to the individual, wherein the block copolymer comprises a labeling moiety, and

b) determining the distribution of the block copolymer in its disassociated form.

74 .- 75 . (canceled)

76 . A method for delivery of a drug or imaging agent to early endosomes, comprising administration of a composition of claim 42 to an individual in need thereof, wherein the micelle (i) encapsulates said drug or imaging agent and (ii) has a pH transition value of about 5.9 to about 6.5.

77 . A method for delivery of a drug or imaging agent to late endosomes or lysosomes, comprising administration of a composition of claim 42 , to an individual in need thereof, wherein the micelle (i) encapsulates said drug or imaging agent and (ii) has a pH transition value of about 5.0 to about 5.5.

78 .- 80 . (canceled)

81 . A compound of the formula:

82 . A compound of the formula:

83 . A compound of the formula:

84 .- 91 . (canceled)

92 . The method of claim 76 , further comprising determining the distribution of the block copolymer in its disassociated form.

93 . The method of claim 79 , further comprising determining the distribution of the block copolymer in its disassociated form.