Hyperbranched polymeric micelles for encapsulation and delivery of hydrophobic molecules
First Claim
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1. A polymer having a structure selected from the group consisting of:
- R(—
O—
R1), and R(—
NH—
R1)x wherein R(—
O—
)x is a polyol moiety and R(—
NH)x is a polyamine moiety, with x being between 2 and 10, inclusive, and each R1 independently has the structure;
wherein
is a divalent amino acid moiety with R2 being a covalent bond or having from 1 to 8 carbon atoms, and y and z are between 0 and 10, inclusive, provided that y and z are not both 0;
wherein
is a divalent dicarboxylic acid moiety in which R3 is an alkylene or cycloalkylene group containing from 1 to about 15 carbon atoms, substituted with a total of from 1 to about 10 hydroxyl groups, with at least a portion of the hydroxyl groups being acylated with from 3 to about 24 carbon atom carboxylic acids; and
wherein R4 is a poly(alkylene oxide) having the structure;
R5—
(R6—
O—
)a—
R6-Q- with R5 being selected from the group consisting of 1 to 40 carbon atom alkyl groups, —
OH, —
OR7, —
NH2, —
NHR7, —
NHR7R8, —
C—
OH, —
C—
OR7, —
C—
O—
C—
R7, —
C—
NH2, —
C—
NHR7 and —
C—
NR7R8;
R6, R7 and R8 being independently selected from the group consisting of 2 to 40 carbon atom, straight-chain or branched alkylene groups;
Q being a divalent linkage moiety; and
a being between 2 and 110, inclusive;
with the proviso that when y is 0 and R is a 1,1,1-tris(hydroxyphenyl)ethane moiety, the divalent dicarboxylic acid moiety is not an acylated mucic acid moiety.
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Abstract
Polymeric micelles for encapsulation of hydrophobic molecules are provided. Methods and formulations for delivering hydrophobic molecules to a host via these micelles are also provided. Methods of stabilizing liposomes or lipid based formulations by addition of polymeric micelles are also provided.
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Citations
36 Claims
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1. A polymer having a structure selected from the group consisting of:
R(—
O—
R1), and R(—
NH—
R1)xwherein R(—
O—
)x is a polyol moiety and R(—
NH)x is a polyamine moiety, with x being between 2 and 10, inclusive, and each R1 independently has the structure;
wherein
is a divalent amino acid moiety with R2 being a covalent bond or having from 1 to 8 carbon atoms, and y and z are between 0 and 10, inclusive, provided that y and z are not both 0;
wherein
is a divalent dicarboxylic acid moiety in which R3 is an alkylene or cycloalkylene group containing from 1 to about 15 carbon atoms, substituted with a total of from 1 to about 10 hydroxyl groups, with at least a portion of the hydroxyl groups being acylated with from 3 to about 24 carbon atom carboxylic acids; and
wherein R4 is a poly(alkylene oxide) having the structure;
R5—
(R6—
O—
)a—
R6-Q-with R5 being selected from the group consisting of 1 to 40 carbon atom alkyl groups, —
OH, —
OR7, —
NH2, —
NHR7, —
NHR7R8, —
C—
OH, —
C—
OR7, —
C—
O—
C—
R7, —
C—
NH2, —
C—
NHR7 and —
C—
NR7R8;
R6, R7 and R8 being independently selected from the group consisting of 2 to 40 carbon atom, straight-chain or branched alkylene groups;
Q being a divalent linkage moiety; and
a being between 2 and 110, inclusive;
with the proviso that when y is 0 and R is a 1,1,1-tris(hydroxyphenyl)ethane moiety, the divalent dicarboxylic acid moiety is not an acylated mucic acid moiety. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 36)
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14. A hydrophobic molecule encapsulated in a polymer, said polymer having a structure selected from the group consisting of:
R(—
O—
R1)x and R(—
NH—
R1)xwherein R(—
O—
)x is a polyol moiety and R(—
NH—
)x is a polyamine moiety, with x being between 2 and 10, inclusive, and each R1 independently has the structure;
wherein
is a divalent amino acid moiety with R2 being a covalent bond or having from 1 to 8 carbon atoms, and y and z are between 0 and 10, inclusive, provided that y and z are not both 0;
wherein
is a divalent dicarboxylic acid moiety in which R3 is an alkylene or cycloalkylene group containing from 1 to about 15 carbon atoms, substituted with a total of from 1 to about hydroxyl groups, with at least a portion of the hydroxyl groups being acylated with from 3 to about 24 carbon atom carboxylic acids; and
wherein R4 is a poly(alkylene oxide) having the structure;
R5—
(—
R6—
O—
)a—
R6-Qwith R5 being selected from the group consisting of 1 to 40 carbon atom alkyl groups, —
OH, —
OR7, —
NH2, —
NHR7, —
NHR7R8, —
C—
OH, —
C—
OR7, —
C—
O—
C—
R7, —
C—
NH2, —
C—
NHR7, and —
C—
NR7R8;
R6, R7 and R8 being independently selected from the group consisting of 2 to 40 carbon atom, straight-chain or branched alkylene groups;
Q being a divalent linkage moiety; and
a being between 2 and 110, inclusive;
with the proviso that when y is 0 and R is a 1,1,1-tris (hydroxyphenyl)ethane moiety, the divalent dicarboxylic acid moiety is not a mucic acid moiety acylated with carboxylic acids having less than 6 carbon atoms. - View Dependent Claims (15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35)
Specification