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Compositions comprising a photosensitizer and a skin-penetration enhancer and their use in photodynamic treatment

a technology of skin penetration enhancer and photosensitizer, which is applied in the direction of radiation therapy, biocide, pharmaceutical non-active ingredients, etc., can solve the problems of difficult formulation of stable composition, local delivery, and difficult penetration of photosensitizing agents into stratum corneum, so as to improve stability and improve the delivery of photosensitizer

Inactive Publication Date: 2005-04-28
QLT INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007] The present invention relates to a composition comprising a photosensitizing agent and at least one skin-penetration enhancer. The compositions herein show improved delivery of the photosensitizer through the stratum corneum. In addition, the compositions of the present invention show improved stability.
[0008] The photosensitizers of the present compositions are able to penetrate the stratum corneum. Consequently, when light energy is delivered, the photosensitizer is activated at the target tissue rather than at the surface. This means that the compositions are more efficacious. In addition, it has surprisingly been found that, when using the compositions of the present invention, administration of light does not cause substantial skin photosensitivity. While not wishing to be bound by theory, it is thought that this the fact that the photosensitizer distributes to the epidermis, rather than in the dermis, means there is less skin photosensitivity.

Problems solved by technology

However, local delivery also has some disadvantages.
Photosensitizing agents do not easily penetrate the stratum corneum.
In addition, the PS agents are relatively reactive so it is difficult to formulate a stable composition.
The solution containing dissolved drug must be discarded two hours after mixing due to the short stability of the product
It has also been found that topical photosensitizer compositions can cause skin-photosensitivity reactions.
In addition, it has been problematic to deliver the photosensitizer to the correct target tissue because often the stratum corneum is difficult to penetrate.

Method used

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  • Compositions comprising a photosensitizer and a skin-penetration enhancer and their use in photodynamic treatment
  • Compositions comprising a photosensitizer and a skin-penetration enhancer and their use in photodynamic treatment

Examples

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[0062] It will be understood that the following embodiments of the present invention are intended to be illustrative of some of the possible applications or principles. Various modifications may be made by the skilled person without departing from the true spirit and scope of the invention.

Example 1Example 2Example 3Comparative(wt %)(wt %)(wt %)Example (wt %)QLT00740.50.250.750.5PEG-20054505854Transcutol ®12024160PEG-335015.51015.515.5Oleyl Alcohol1015.751030

1Diethylene glycol monethyl ether available from Gattefosse Canada Inc., Baie D'Urfé, Québec, H9X 2T3, Canada

[0063] The above compositions were prepared in the following way: [0064] a) Preparation of cryodessicated photosensitizer—the QLT0074 is dissolved in Glacial Acetic Acid. The solution is then frozen in a dry icelisopropanol bath and the acetic acid is removed by lyophilization. The resultant material is a fine fluffy powder which goes into topical solution easily. [0065] b) Manufacture of base—the PEG 200 is warmed to ...

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Abstract

The present invention relates to a composition comprising a photosensitizing agent and a skin-penetration enhancer. The composition herein show improved delivery of the photosensitizer through the stratum corneum. In addition, the composition of the present invention show improved stability and a reduced incidence of skin photosensitivity.

Description

TECHNICAL FIELD [0001] The present invention relates to a composition comprising photosensitizing agents. BACKGROUND OF THE INVENTION [0002] Photodynamic therapy is a diverse field of medical treatment. Generally, PDT involves the delivery of a photosensitizer to the target tissue and, subsequently, irradiating the target area with light of an appropriate wavelength to activate the PS. This activation results in an agent that modifies or destroys the target tissues. The PS is usually delivered systemically although it has been proposed to deliver it locally. [0003] Local delivery has the advantage that the PS is delivered directly to the target tissue and, consequently, high concentrations of the drug in the target tissue can be achieved. However, local delivery also has some disadvantages. Photosensitizing agents do not easily penetrate the stratum corneum. In addition, the PS agents are relatively reactive so it is difficult to formulate a stable composition. [0004] At the time of...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/49A61K9/00A61K31/40A61K31/409A61K41/00A61K47/10A61N5/06A61P17/14A61P43/00A61Q7/00
CPCA61K8/4913A61K9/0014A61K9/0019A61K31/40A61K31/555A61K41/0071A61K2800/434A61K2800/81A61N5/0617A61N5/062A61Q7/00A61K47/10A61P15/08A61P17/00A61P17/06A61P17/10A61P17/14A61P35/00A61P37/08A61P43/00
Inventor BOCH, RONALD ERWINLUTWYCHE, PETERNORTH, JOHN ROBERTMONK, WENDY
Owner QLT INC
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