Method for providing an active agent topically to the skin

a technology of active agents and skin, applied in the direction of aerosol delivery, inorganic non-active ingredients, extracellular fluid disorder, etc., can solve the problem that the transdermal drug delivery system has not been integrated into the application of topical dressings, and achieve the effect of accelerating wound healing and enhancing the release of active agents

Inactive Publication Date: 2007-08-16
DANISCO US INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007] In accordance with one aspect of the present invention, the preparation may comprise a thin film dressing that can be applied over the skin, including damaged tissue. In accordance with another aspect of the present invention, the preparation comprises a patch dressing. In accordance with still another aspect of the present invention, the preparation comprises a spread-on bandage dressing. In accordance with another aspect of the present invention, the preparation comprises an ointment. The thin film, the patch, the spread-on bandage, and the ointment can all be applied to the skin, over a surgical incision, a wound, or other skin lesion, abrasion, scrape, scratch, or other damaged tissue. The preparations may be occlusive to liquids and are effective in blocking microorganisms that cause infection from the skin surface. In one embodiment, active agents, such as protease, can be released from the preparations at the site of a wound for enzymatic debridement, clotting formation and clot removal, as well as in situ peroxide and / or peracid generation to accelerate wound healing at different stages thereof.
[0008] In a preferred embodiment, the topical preparation comprises a mixture of a hydrophilic carrier containing an active agent that is dispersed throughout a silicone matrix. The mixture together with the silicone matrix forms the topical preparation of this embodiment of the present invention. The hydrophilic carrier is, for example, a solution of propylene glycol, which may be mixed with a water soluble or hydrophilic component such as, for example, polyvinyl alcohol (“PVA”) or polyvinylpyrrolidone (“PVP”). The hydrophilic carrier and active agent mixture may form an internal phase that is an emulsion or dispersion, and this internal phase is disposed within the silicone matrix (external phase). Consequently, a silicone-based surfactant can be added to disperse or emulsify the internal phase into very small droplets and enhance the release of active agent.

Problems solved by technology

However, these transdermal drug delivery systems have not been incorporated into topical dressing applications such as wound dressings and ointments, wherein a biochemical agent dispersed within a silicone matrix is released onto skin or a wound to accelerate healing.

Method used

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  • Method for providing an active agent topically to the skin
  • Method for providing an active agent topically to the skin
  • Method for providing an active agent topically to the skin

Examples

Experimental program
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example 1

[0065] A first experiment was conducted to evaluate the sustained release of protease from a silicone matrix. A loosely or lightly cross-linked silicone elastomer composition (Dow Corning® 9040) and a silicone-based surfactant (Dow Corning® 9011), both commercially available from Dow Corning Corporation (Midland, Mich.), were used to form a Dow Corning® 9040 and a Dow Corning® 9040 / 9011 silicone elastomer formulation. A 1.1 mg / ml protease A, derived from =i B. lentus=l , stock solution dissolved in propylene glycol was added to both Dow Corning® compositions. A 5 ml. sample of the stock solution was added to 20 grams of the 9040 formulation and also to 20 grams of the 9040 / 9011 formulation, which comprises 10 grams of the 9040 formulation and 10 grams of the 9011 formulation. Controls comprising 9040 and 9040 / 9011 plus water instead of the stock enzyme solution were prepared. In addition, to determine whether any component of the silicone matrix was inhibiting the protease, further ...

example 2

[0067] Another experiment was conducted to evaluate the sustained release of protease from a silicone matrix. A 0.5 ml aliquot of 0.81 mg / ml Protease A in polyethylene glycol stock solution was transferred into a small polypropylene weighing boat. Next, 5.0 ml of a silicone rubber composition (Dow Corning® 7-5300 from Dow Corning Corporation, Midland, Mich.) was added to the protease solution and mixed within 15 seconds of its addition. It is contemplated that the Dow Corning® 7-5300 composition has applications as a “spread-on” film, patch, or bandage. The mixture was then allowed to cure for 30 minutes. Following curing, the mixture was washed three times using 1.0 ml of distilled water. Each wash was assayed using the SAAPFpNA assay on the aliquots, as referenced above, and the amount of enzyme in the wash was measured. The composition was then dried on its side for 15 minutes, followed by an additional 15 minutes laying flat. Finally, 5.0 ml of distilled water was added to the w...

example 3

[0071] Still another experiment was conducted to evaluate the effect of hydrophilic additives on the sustained release of Protease A from a silicone matrix. First, test dressings or, more specifically, patches containing protease were cast into small petri-dishes (approximately 3 cm in diameter) such that the total weight of the patches was constant (about 2 grams) and the concentration of enzyme in the patches was also constant (about 0.6 mg agent per gram of patch). The patches were comprised of a loosely or lightly cross-linked silicone elastomer composition (Dow Corning® 9040) and a silicone-based surfactant (Dow Corning® 9011), both commercially available from Dow Corning Corporation (Midland, Mich.). In addition, Dow Corning® 7-5300 (a silicone rubber composition) was also tested. Additionally, the formulations contained varying amounts of PVA, PVA at high propylene glycol levels, or PVP that were added by stirring.

[0072] Enzyme release was evaluated using two methods. In the...

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Abstract

A method of providing an active agent topically to the skin is provided and includes providing a topical preparation having an internal phase and an external phase, wherein the internal phase is dispersed within the external phase. The internal phase includes at least one hydrophilic carrier, at least one hydrophilic component, and at least one active agent, and the external phase comprises a silicone matrix. The topical preparation is placed in contact with the skin of a patient such that the active agent is released from the silicone matrix topically onto the skin of the patient.

Description

CROSS REFERENCES TO RELATED APPLICATIONS [0001] The present application is a continuation of U.S. patent application Ser. No. 10 / 660,101 filed Sep. 10, 2003, which claims priority to U.S. patent application Ser. No. 10 / 385,213, filed Mar. 10, 2003, which claims priority to U.S. Provisional Patent Application No. 60 / 363,386, filed Mar. 11, 2002 and U.S. Provisional Patent Application No. 60 / 439,862, filed Jan. 14, 2003.BACKGROUND OF THE INVENTION [0002] The present invention relates in general to methods for supplying an active agent for topical skin treatment and, more particularly, to methods of using preparations comprising silicone matrices and hydrophilic carriers that provide sustained release of active agents when applied to the skin. [0003] Silicones are compounds based on alkylsiloxane or organosiloxane chemistry and include polydimethylsiloxane materials that have been used as excipients and process aids in pharmaceutical applications. Some of these materials have attained ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K9/06A61K9/00A61K9/70A61K38/16A61K38/18A61K38/19A61K38/43A61K38/46A61K38/48A61K47/10A61K47/24A61K47/34A61L26/00A61P7/02A61P7/12
CPCA61K9/0014A61K38/465A61K9/7069A61K38/482A61K47/02A61K47/24A61K47/34A61L26/0019A61L26/0066A61L2300/254A61L2300/602A61L2300/622A61K9/7007C08L83/04A61P17/02A61P7/02A61P7/12A61K47/38A61K38/43
Inventor BOTT, RICHARD R.GEBERT, MARK S.KLYKKEN, PAAL CHRISTIANMAZEAUD, ISABELLETHOMAS, XAVIER JEAN-PAUL
Owner DANISCO US INC
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