# US 2014/0193504 A1 · Polymer-drug systems

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- Number: US 2014/0193504 A1
- Document ID: US20140193504A1
- Status: Published application
- Kind: A1
- Application number: 14/043,456
- Filed: 2013-10-01
- Published: 2014-07-10
- Earliest claimed: 2013-01-04
- Assignees: The Texas A&M University System
- Inventors: Karen Wooley; Jiong Zou; Mahmoud El Sabahy; Shiyi Zhang; Fuwu Zhang
- Web page: https://patentgrep.com/patent/US20140193504A1

## CPC

- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 47/59: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K 47/593: {Polyesters, e.g. PLGA or polylactide-co-glycolide}
- A61P 35/00: Antineoplastic agents
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure generally relates to polymer-drug systems, and more particularly to nanoscopic particles comprising amphiphilic block copolymers conjugated, physically encapsulated, or otherwise combined with chemotherapeutic agents along a selective region or regions of the backbone of the copolymer, so as to package the chemotherapeutic agent in selective domains within each nanoscopic particle, as well as to methods for making such particles, and applications and methods for using such particles, including in the formation of polymer micelles.

## Claims

### Claim 1

A composition comprising:
an amphiphilic block copolymer comprising a polymer backbone, and
a chemotherapeutic agent.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the block copolymer comprises a hydrophilic copolymer and a second copolymer segment.

### Claim 3 (depends on 2)

The composition of claim 2, wherein the second copolymer segment comprises a degradable polyphosphoester.

### Claim 4 (depends on 3)

The composition of claim 3, wherein the degradable polyphosphoester comprises a reactive side chain functionality.

### Claim 5 (depends on 4)

The composition of claim 4, wherein the reactive side chain functionality is able to undergo a click-type chemical reaction.

### Claim 6 (depends on 5)

The composition of claim 5, wherein the reactive side chain functionality is selected from the group consisting of: an alkynyl and an alkenyl.

### Claim 7 (depends on 3)

The composition of claim 3, wherein the block copolymer is conjugated with the chemotherapeutic agent.

### Claim 8 (depends on 3)

The composition of claim 3, wherein the block copolymer encapsulates the chemotherapeutic agent.

### Claim 9 (depends on 7)

The composition of claim 7, wherein the chemotherapeutic agent is conjugated with the copolymer along a selective region of the polymer backbone.

### Claim 10 (depends on 9)

The composition of claim 9, wherein the chemotherapeutic agent comprises paclitaxel (PTX).

### Claim 11 (depends on 10)

The composition of claim 10, further comprising a functional group selected from the following group: an ester, a disulfide, and thiopropionate.

### Claim 12 (depends on 11)

The composition of claim 11, wherein the functional group is β-thioproprionate.

### Claim 13 (depends on 10)

The composition of claim 10, further comprising a pendant compound selected from the following group: a dye, an imaging agent, and a hydrophilic polymer, wherein the pendant compound is chemically reacted with the polyphosphoester via the functional group of the polyphosphoester.

### Claim 14 (depends on 1)

The composition of claim 1 wherein the block copolymer is a diblock copolymer.

### Claim 15 (depends on 1)

The composition of claim 1 wherein the block copolymer is a multi-block copolymer.

### Claim 16

A composition comprising:
a block copolymer comprising a hydrophobic-functional AB diblock polyphosphoester; and
a chemotherapeutic agent.

### Claim 17 (depends on 16)

The composition of claim 16, wherein the a hydrophobic-functional AB diblock polyphosphoester is unmodified.

### Claim 18 (depends on 16)

The composition of claim 16, wherein the a hydrophobic-functional AB diblock polyphosphoester is modified with a functionality comprising an anionic, cationic, zwitterionic, or neutral moiety or a combination thereof

### Claim 19 (depends on 18)

The composition of claim 18, wherein the block copolymer is derived from poly(ethylbutyl phospholane)-block-poly (butynyl phospholane) (PEBP-b-PBYP).

### Claim 20 (depends on 16)

The composition of claim 16, comprising a plurality of hydrophobic AB diblock polyphosphoesters modified with a functionality comprising an anionic, cationic, zwitterionic, or neutral moiety or a combination thereof.

### Claim 21 (depends on 16)

The composition of claim 16, wherein the wherein the composition comprises poly(ethylbutyl phospholane)-block-poly (butynyl phospholane)-graft-polyethylene glycol (PEBP-b-PBYP-g-PEG).

### Claim 22 (depends on 16)

The composition of claim 16, wherein the block copolymer encapsulates the chemotherapeutic agent.

### Claim 23 (depends on 16)

The composition of claim 16, wherein the chemotherapeutic agent comprises paclitaxel (PTX).