Photokinetic delivery of biologically active substances using pulsed incoherent light

• US 7,854,753 B2
• Filed: 06/30/2008
• Issued: 12/21/2010
• Est. Priority Date: 10/04/2002
• Status: Active Grant

• Current Assignee: Photokinetix, Inc.
• Original Assignee: Photokinetix, Inc.
• Inventors: Kraft, Edward R., Kulp, Gabriela
• Primary Examiner(s): Desai; Anand U
• Application Number:
  US12/215,899
• Publication Number:
  US 20090156463A1
• Time in Patent Office: 904 Days
• Field of Search: None
• US Class Current: 607/88
• CPC Class Codes: A61K 41/0042 Photocleavage of drugs in vivo, e.g. cleavage of photolabile linkers in vivo by UV radiation for releasing the pharmacologically-active agent from the administered agent; photothrombosis or photoocclusion
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00

Abstract

The invention relates generally to transdermal and transmembrane delivery of biologically active substances through the skin, sub-dermal tissues, blood vessels and cellular membranes without causing damage to the cellular surface, tissue or membrane. The invention provides compositions and methods for enhanced transdermal and transmembrane delivery of biologically active substances using pulsed incoherent light. The invention further provides a device for the application of the pulsed incoherent light to cellular surfaces and membranes using those compositions and methods.

Claims

1. A composition for photokinetic delivery of a biologically active substance using pulsed incoherent light, comprising a biologically active substance, a solvent, a gelling agent and a photocatalytic agent, wherein said photocatalytic agent has a band gap energy of between about 2.9 eV and about 3.2 eV.

2. The composition according to claim 1, wherein said photocatalytic agent is present in said composition at a concentration of between 0.001% and 20% (w/w).

3. The composition according to claim 1, wherein said photocatalytic agent is present in said composition at a concentration of 2% (w/w).

4. The composition according to claim 1, wherein said biologically active substance is present in said composition at a concentration of between 0.01% and 2% (w/v).

5. The composition according to claim 1, wherein said biologically active substance is present in said composition at a concentration of between 0.05% and 1% (w/v).

6. The composition according to claim 1, wherein said gelling agent is present in said composition at a concentration of between 0.1% and 10% (w/v).

7. The composition according to claim 1, wherein said gelling agent is present in said composition at a concentration of 1% (w/v).

8. The composition according to claim 1, wherein the biologically active substance is a polar compound selected from the group consisting of theophylline-7 acetic acid, sodium ascorbyl phosphate, ascorbic acid, ascorbyl palmitate, pyridoxine, and nicotinic acid.

9. The composition according to claim 1, wherein the biologically active substance is a non-polar compound selected from the group consisting of theobromine, theophylline, caffeine, and nicotinamide.

10. The composition according to claim 1, wherein the biologically active substance is selected from the group consisting of an analgesic, an anaesthetic, an antacid, an antianxiety drug, an antiarrhythmic, an antibacterial, an antibiotic, an anticoagulant and thrombolytic, an anticonvulsant, an antidepressant, an antidiarrheal, an antiemetic, an antifungal, an antihistamine, an antihypertensive, an anti-inflammatory, an antieoplastic, an antipsychotic, an antipyretic, an antiviral, a barbiturate, a beta-blocker, a bronchodilator, a cold cure, a corticosteroid, a cough suppressant, a cytotoxic, a decongestant, a diuretic, an expectorant, a hypoglycemic, an immunosuppressive, a laxative, a muscle relaxant, a sedative, a sex hormone, a sleeping drug, a tranquilizer, and a vitamin.

11. The composition according to claim 1, wherein the biologically active substance is selected from the group consisting of an analgesic, an anaesthetic, an antacid, an antianxiety drug, an antiarrhythmic, an antibacterial, an antibiotic, an anticoagulant and thrombolytic, an anticonvulsant, an antidiarrheal, an antiviral, a barbiturate, a cytotoxics, and a vitamin.

12. The composition according to claim 1, wherein the biologically active substance is an anaesthetic.

13. The composition according to claim 12, wherein the anaesthetic is lidocaine.

14. The composition according to claim 1, wherein said biologically active substance is a peptide.

15. The composition according to claim 14, wherein the peptide is selected from the group consisting of Gly-Tyr, Val-Tyr-Val, Tyr-Gly-Gly-Phe-Met (SEQ ID NO:

1), Tyr-Gly-Gly-Phe-Leu (SEQ ID NO;

     2), and Asp-Arg-Val-Tyr-Ile-His-Pro-Phe (SEQ ID NO;

     3).

16. The composition according to claim 1, wherein said biologically active substance is a hormone.

17. The composition according to claim 16, wherein the hormone is selected from the group consisting of methionine enkephalin acetate, leucine enkephalin, angiotensin II acetate, β

-estradiol, methyl testosterone, progesterone and insulin.

18. The composition according to claim 1, wherein said biologically active substance is a protein.

19. The composition according to claim 18, wherein the protein is selected from the group consisting of an enzyme, an antibody, and a glycoprotein.

20. The composition according to claim 1, wherein said biologically active substance is an antibiotic.

21. The composition according to claim 20, wherein the antibiotic is amphotericin B.

22. The composition according to claim 1, wherein said gelling agent is selected from the group consisting of hydroxypropyl cellulose, hydroxyethyl cellulose, agar, pectine, alginic acid and its salts, guar gum, polyvinyl alcohol, polyethylene oxide, cellulose and its derivatives, propylene carbonate, polyethylene glycol, hexylene glycol sodium carboxymethylcellulose, polyacrylates, polyoxyethylene-polyoxypropylene block copolymers, pluronics, wood wax alcohols and tyloxapol.

23. The composition according to claim 22, wherein said gelling agent is hydroxypropyl cellulose.

24. The composition according to claim 1, wherein said photocatalytic agent is selected from the group consisting of a rutile form of titanium dioxide, an anatase form of titanium dioxide, a brookite form of titanium dioxide, ZnO, ZrO₂ and Sc₂O₃.

25. The composition according to claim 24, wherein said photocatalytic agent is a rutile form of titanium dioxide.

26. The composition according to claim 1, wherein said solvent is an aqueous or an organic solvent.

27. The composition according to claim 26, wherein the solvent is water.

28. The composition according to claim 26, wherein the solvent is an aqueous solution of ethyl lactate or propylene glycol or both.