# US 7,744,919 B2 · Block copolymer micelle composition having an enhanced drug-loading capacity and sustained release

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- Number: US 7,744,919 B2
- Document ID: US7744919B2
- Status: Granted
- Kind: B2
- Application number: 10/526,836
- Filed: 2003-05-30
- Published: 2005-12-29
- Granted: 2010-06-29
- Earliest claimed: 2002-09-04
- Assignees: Postech Foundation
- Inventors: Kilwon Cho; Jae Young Lee
- Web page: https://patentgrep.com/patent/US7744919B2

## CPC

- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- 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)

## Abstract

A micelle drug composition having an enhanced drug-loading capacity and improved sustained-release characteristics comprising an amphiphilic block copolymer including at least one hydrophilic blocks and at least one hydrophobic blocks. The block copolymer comprises functional groups selected from the group consisting of carboxyl, amine, hydroxyl, amide, thiol and sulfonic acid groups, in the hydrophobic block chain of the copolymer, and the average number of the functional groups range from 1.1 to 30.

## Claims

### Claim 1

A micelle composition for drug deliver system comprising an amphiphilic block copolymer represented by formula (1):
wherein R1 is H, C1-4 alkyl or C1-4 acyl;
R2 is H, C1-9 alkyl, aryl or C1-9 arylalkyl;
x is a number ranging from 10 to 400;
y is a number ranging from 10 to 300;
z is a number ranging from 1.1 to 30;
a ratio, z/y ranges from 0.015 to 2; and
W is selected from the group consisting of carboxyl, amine, hydroxyl, amide, thiol and sulfonic acid groups.

### Claim 2 (depends on 1)

The composition of claim 1, wherein W is a carboxyl group.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the ratio z/y ranges from 0.02 to 1.5.

### Claim 4 (depends on 1, 2, 3)

A pharmaceutical micelle composition comprising a hydrophobic drug introduced in the micelle composition according to any one of claims 1, 2 and 3.

### Claim 5 (depends on 4)

The composition of claim 4, wherein the drug is selected from the group consisting of paclitaxel, camptothecin, biphenyl dimethyl dicarboxylate, piposulfan, danazole, taxotere, adriamycin, indomethacin, etoposide, itraconazole, nystatin, and omeprazole.

### Claim 6 (depends on 4)

The composition of claim 4, wherein the drug is present in an amount ranging from 0.1 to 5% by weight, based on the total night of the micelle composition.