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US 2003/0152630 A1Published application
PEG-POE, PEG-POE-PEG, and POE-PEG-POE block copolymers
OwnerSteven Y. Ng, Jorge Hellerinventors
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Abstract
PEG-POE, PEG-POE-PEG, and POE-PEG-POE block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents, especially when the POE block(s) contain at least one unit containing an α-hydroxy acid.
Claims20
A block copolymer of formula X, formula Y, or formula Z:
- R1—[OCH2CH2]f—[POE]g—H (X),R1—[OCH2CH2]f—[POE]g—[OCH2CH2]h—OR2 (Y),H—A—[POE]g—[OCH2CH2]h—[POE]j—H (Z),
- where:
- R1 is C1-4 alkyl;
- R2 is C1-4 alkyl;
- f and h are independently an integer from 2 to 1000;
- g and j are independently an integer from 2 to 200;
- POE is a poly(ortho ester) of formula I or formula II:
- 16
- where:
- R3 is a bond, —(CH2)a—, or —(CH2)b—O—(CH2)c—;
- where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5;
- R4 is a C1-4 alkyl;
- and
- each A is R5, R6, or R7, where
- R5 is:
- 17
- where:
- p is an integer of 1 to 20;
- R8 is hydrogen or C1-4 alkyl;
- and
- R9 is:
- 18
- where:
- s is an integer of 0 to 30;
- t is an integer of 2 to 20;
- and
- R10 is hydrogen or C1-4 alkyl;
- R6 is:
- 19
- R7 is a diol containing at least one functional group independently selected from amide, imide, urea, and urethane groups;
- where A is R7 in at least 0.1 mol % of the POE units when the poly(ortho ester) is of formula I.
28 more elements
Dependencies are inferred from the claim text.