MICROSPHERES FOR ACTIVE EMBOLIZATION

• US 20120141379A1
• Filed: 02/13/2012
• Published: 06/07/2012
• Est. Priority Date: 03/24/2000
• Status: Active Grant

• Current Assignee: Biosphere Medical Inc. (Merit Medical Systems, Inc.)
• Original Assignee: Biosphere Medical Inc. (Merit Medical Systems, Inc.)
• Inventors: Vogel, Jean-Marie, Boschetti, Egisto
• Granted Patent: US 8,741,351 B2
• Time in Patent Office: Days
• US Class Current: 424/9.3
• CPC Class Codes: A61K 31/715 Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61L 2430/36 for embolization or occlusion, e.g. vaso-occlusive compositions or devices artificial blood vessels A61L27/507
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/04 specific for metastasis
• CPC Class Codes: A61P 41/00 Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
• CPC Class Codes: Y10T 428/2982 Particulate matter [e.g., sphere, flake, etc.]

Abstract

The present invention relates to injectable compositions comprising biocompatible, swellable, substantially hydrophilic, non-toxic and substantially spherical polymeric material carriers which are capable of efficiently delivering bioactive therapeutic factor(s) for use in embolization drug therapy. The present invention further relates to methods of embolization gene therapy, particularly for the treatment of angiogenic and non-angiogenic-dependent diseases, using the injectable compositions.

Claims

1. A microsphere suitable for active embolization, comprising:

a substantially spherical and biocompatible copolymer of sodium acrylate and vinyl alcohol, and

doxorubicin.

2. The microsphere of claim 1, wherein the doxorubicin is associated with the copolymer by an ionic interaction.

3. The microsphere of claim 1, wherein the microsphere is cross-linked and swellable.

4. The microsphere of claim 1, wherein the copolymer comprises from about 0.5% to about 20% of crosslinking bridges.

5. The microsphere of claim 1, wherein the doxorubicin is contained within the microsphere.

6. The microsphere of claim 1, wherein the doxorubicin is adsorbed or absorbed by the microsphere.

7. The microsphere of claim 1, wherein the diameter of the microsphere ranges from about 10 μ

m to about 2000 μ

m.

8. The microsphere of claim 3, wherein the diameter of the microsphere ranges from about 10 μ

m to about 400 μ

m before swelling.

9. The microsphere of claim 3, wherein the diameter of the microsphere ranges from about 10 μ

m to about 2000 μ

m after swelling.

10. An injectable composition comprising the microsphere of claim 1 and a biocompatible carrier, wherein the composition is sterile.

11. The composition of claim 10, wherein the composition comprises the microsphere in an amount from about 10% to about 50% by weight and the biocompatible carrier in an amount from about 50% to about 90% by weight.

12. The composition of claim 10, wherein the biocompatible carrier comprises a salt composed of cations selected from the group consisting of sodium, potassium, calcium, magnesium, iron, zinc, ammonium, and mixtures thereof, in an amount of from about 0.01 M to about 5 M.

13. The composition of claim 10, further comprising a fluorescent marker, chemical dye, contrast agent, magnetic resonance imaging agent, or a mixture thereof.

14. The composition of claim 10 where the composition is injectable through a needle of about 18 gauge or smaller.

15. A microsphere suitable for active embolization, comprising:

a substantially spherical and swellable, biocompatible anionic copolymer of sodium acrylate and vinyl alcohol, and

a positively-charged drug.

16. The microsphere of claim 15, wherein the drug is associated with the copolymer by an ionic interaction.

17. The microsphere of claim 15, wherein the drug is a neoplastic agent.

18. The microsphere of claim 15, wherein the drug is doxorubicin.

19. The microsphere of claim 15, wherein the microsphere is cross-linked.

20. The microsphere of claim 15, wherein the copolymer comprises from about 0.5% to about 20% of crosslinking bridges.

21. The microsphere of claim 15, wherein the diameter of the microsphere ranges from about 10 μ

m to about 2000 μ

m.