POLYMERIC MICELLES FOR COMBINATION DRUG DELIVERY
First Claim
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1. A block polymer comprising a first block and a second block;
- whereinthe first block comprises two or more ethylene glycol segments;
the second block comprises two or more amino acid units derived from aspartic acid, glutamic acid, or a combination of aspartic acid and glutamic acid;
two or more amino acid side chains of the second block are individually covalently linked to therapeutic agents through hydrazide moieties; and
the therapeutic agents comprise at least two different therapeutic agents.
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Abstract
The invention provides block polymers, micelles, and micelle formulations for combination drug therapy. Polyamide block polymers, such as those of formulas I and II are useful, for example, for preparation of mixed drug micelles, including simply mixed micelles, physically mixed micelles, and chemically mixed micelles. The invention further provides methods of treating cancer, and inhibiting and killing cancer cells. Also provided are methods for the preparation of polymer drug conjugates and intermediates for their synthesis.
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Citations
23 Claims
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1. A block polymer comprising a first block and a second block;
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wherein the first block comprises two or more ethylene glycol segments; the second block comprises two or more amino acid units derived from aspartic acid, glutamic acid, or a combination of aspartic acid and glutamic acid; two or more amino acid side chains of the second block are individually covalently linked to therapeutic agents through hydrazide moieties; and the therapeutic agents comprise at least two different therapeutic agents. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 16)
wherein the first block comprises about 10 to about 600 ethylene glycol segments; the second block comprises 5 to about 100 amino acid units derived from aspartic acid, glutamic acid, or a combination of aspartic acid and glutamic acid; and two or more side chains of the second block are covalently linked to a therapeutic agent through a linker of the formula;
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16. A micelle comprising a plurality of polymers of claim 1, wherein the therapeutic agents reside toward the core of the micelle and the ethylene glycol segments of the polymers align toward the corona of the micelle.
- 13. A polymer comprising formula I:
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17. A micelle formulation comprising a plurality of block polymers comprising a first block and a second block;
wherein the first block comprises two or more ethylene glycol segments; the second block comprises two or more amino acid units derived from aspartic acid, glutamic acid, or a combination of aspartic acid and glutamic acid; at least one amino acid side chain of the second block is covalently linked to a therapeutic agent through a hydrazide moiety; and the micelles of the formulation comprise at least two different therapeutic agents. - View Dependent Claims (18, 19, 20, 21, 22, 23)
Specification