POLYMER MICELLES CONTAINING ANTHRACYLINES FOR THE TREATMENT OF CANCER

• US 20110142950A1
• Filed: 10/29/2010
• Published: 06/16/2011
• Est. Priority Date: 04/30/2009
• Status: Active Grant

• Current Assignee: Intezyne Technologies
• Original Assignee: Intezyne Technologies
• Inventors: Rios-Doria, Jonathan, Skaff, Habib, Sill, Kevin N.
• Granted Patent: US 8,524,784 B2
• Time in Patent Office: Days
• US Class Current: 424/497
• CPC Class Codes: A61K 31/35 having six-membered rings with one oxygen as the only ring hetero atom
• CPC Class Codes: A61K 47/42 Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein oligopeptides having up to five amino acids A61K47/183; polyamino acids A61K47/34
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention provides micelles having an anthracycline encapsulated therein, the micelles comprising a multiblock copolymer. The invention further provides methods of preparing and using said micelles, and compositions thereof.

Claims

1. An anthracycline loaded micelle comprising a multiblock copolymer, wherein said micelle has a drug-loaded inner core, a crosslinked outer core, and a hydrophilic shell, wherein the multiblock copolymer is of formula IX:

2. The micelle according to claim 1, wherein R¹ is —

OCH₃.

3. The micelle according to claim 2, wherein n is 110-450.

4. The micelle according to claim 2, wherein s is 1.

5. The micelle according to claim 2, wherein y is about 20 and z is about 20.

6. The micelle according to claim 1, wherein R¹ is —

N₃.

7. The micelle according to claim 6, wherein n is 110-450.

8. The micelle according to claim 6, wherein s is 1.

9. The micelle according to claim 6, wherein y is about 20 and z is about 20.

10. The micelle according to claim 1, wherein s is 2.

11. The micelle according to claim 1, wherein R¹ is a mixture of —

OCH₃ and

12. The micelle according to claim 11, wherein T is an EGFR targeting peptide.

13. The micelle according to claim 11, wherein T is an uPAR targeting peptide.

14. The micelle according to claim 11, wherein T is a HER2 targeting peptide.

15. The micelle according to claim 1, wherein the anthracycline is daunorubicin.