Transdermal Delivery Using Encapsulated Agent Activated by Ultrasound and or Heat

• US 20110004150A1
• Filed: 09/15/2010
• Published: 01/06/2011
• Est. Priority Date: 12/31/2002
• Status: Active Grant

• Current Assignee: Ultra Sun Technology Inc.
• Original Assignee: Ultra Sun Technology Inc.
• Inventors: Weimann, Ludwig J.
• Granted Patent: US 8,691,268 B2
• Time in Patent Office: Days
• US Class Current: 604/22
• CPC Class Codes: A61K 9/0009 involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis microelectromechanical systems A61K9/0097
• 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
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
• CPC Class Codes: A61K 9/7092 Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs
• CPC Class Codes: A61M 37/00 Other apparatus for introducing media into the body for reproduction or fertilisation A61B17/425; apparatus for iontophoresis or cataphoresis A61N1/30; Percutany, i.e. introducing medicines into the body by diffusion through the skin salt baths A61H33/04
• CPC Class Codes: A61M 37/0092 using ultrasonic, sonic or infrasonic vibrations, e.g. phonophoresis
• CPC Class Codes: A61N 1/30 Apparatus for iontophoresis, i.e. transfer of media in ionic state by an electromotoric force into the body, or cataphoresis

Abstract

A method for delivery of substance through at least one dermal layer, by providing a substance in microcapsules at a predetermined size, within a medium (150) for holding the microcapsules; placing the medium for holding the microcapsules on a surface of a patch (100) adjacent the skin (320) of a human or animal; and applying energy (200) to the patch, the energy having a characteristic of disturbing the integrity of the microcapsules, thereby resulting in release of the substance from the microcapsules. The energy may be selectively applied to release the substance at desired times. The substance may be a drug or other active agent.

Claims

1. A transdermal patch transdermal patch for infusing active substances into an animal body through the skin comprising:

an inner disc, the inner disc including a encapsulated agents in microcapsules, wherein the microcapsules retain the encapsulated agents prior to activation by energy capable of rupturing the microcapsules;

an outer disc for attachment of the patch to the skin, thereby facilitating contact of the inner disc with a surface of the skin.

2. The transdermal patch of claim 1 wherein the active substance to be infused is a pharmaceutical substance and the pharmaceutical substance is retained prior to infusion in a compatible pharmaceutically-acceptable solvent or excipient vehicle, encapsulated in the microcapsules.

3. The transdermal patch of claim 2 wherein the microcapsules are suspended in a suitable composition, such as pressure-sensitive adhesive, adhesive hydrogel, cream and the like, which contains a permeation-enhancing agent and serves as an outer solvent in which the microcapsules are suspended.

4. The transdermal patch of claim 2 wherein the microcapsules are suspended in a suitable composition, such as pressure-sensitive adhesive, adhesive hydrogel, cream and the like, which contains a permeation-enhancing agent and serves as an outer solvent in which the microcapsules are suspended, and the microcapsules are made of a substance or material that does not permit diffusion into or out of the microcapsule and does not allow leaching out of its contents to any significant extent prior to the application of energy.

5. The transdermal patch of claim 4 wherein the driving force of the pharmaceutical substance for delivery transdermally from the external matrix or vehicle such as pressure-sensitive adhesive, adhesive hydrogel, cream and the like, to the skin is proportional to the difference of the solubility parameter between the pharmaceutical substance to be delivered transdermally and the skin, and between the pharmaceutical substance to be delivered transdermally and the external matrix or vehicle.

6. The transdermal patch of claim 5 wherein a difference between the solubility parameters of the substance to be delivered transdermally and the skin in comparison to the difference between the solubility parameters of the substance to be delivered transdermally and the matrix is minimized in order to maintain a high transdermal flux.

7. The transdermal patch of claim 1 wherein the inner disc includes encapsulated agents in microspheres dispersed in hydrogel.

8. The transdermal patch of claim 1 wherein the inner disc includes encapsulated agents in microspheres dispersed in hydrocolloid.

9. The transdermal patch of claim 1 wherein the inner disc includes encapsulated agents in microspheres dispersed in an aqueous medium in a reservoir type patch.

10. The transdermal patch of claim 1 wherein the microspheres have sizes between 0.01 and 100 micrometers.

11. The transdermal patch of claim 1 wherein the microspheres include polymeric shells.

12. The transdermal patch of claim 1 wherein the microspheres are made of liposomes.

13. The transdermal patch of claim 1 wherein the inner disc includes at least one of drug, biologically active compound, excipient, skin permeation enhancer.

14. The transdermal patch of claim 1, wherein said substance includes insulin provided for transdermal delivery.

15. The transdermal patch of claim 1, wherein said substance includes vitamin.

16. The transdermal patch of claim 1, wherein said substance includes skin permeation enhancer.

17. The transdermal patch of claim 1, wherein the medium for holding the microcapsules includes skin permeation enhancer.

18. A vehicle and active substance for delivery of the active substance by transdermally partitioning into the skin from an adhesive matrix of a transdermal patch, wherein the active substance is delivered transdermally dependent on a difference in chemical potentials of the active substance as contained in an external matrix or vehicle and the skin, wherein the active substance is contained within microcapsules which retain the active substance for delivery prior to activation by energy capable of rupturing the microcapsules.

19. The vehicle and active substance of claim 18, wherein the transdermal patch is manufactured in a pre-activated state, thereby providing enhanced storage stability, and control of release characteristics.

20. A device with multiple ultrasound sources for selectively rupturing microparticles in a selected area of a patch.