Site News  |   Monitor Keywords  |   Monitor Archive  |   Organizer  |   Account Info  |

Film-forming resins as a carrier for topical application of pharmacologically active agents

Film-forming resins as a carrier for topical application of pharmacologically active agents description/claims

1. Field of the Invention

The invention relates to resin or other film-forming agent based biological dressings that adhere to the skin and contain one or more pharmacologically active agents for the treatment of symptoms relating to dermatological diseases and those affecting mucous membranes. The invention is exemplified by biological dressings comprising tincture of benzoin and clotrimazole for the treatment of athlete's foot and by biological dressings comprising mastic and ciclopirox for onychomycosis.

2. Background Information

For many forms of dermatological conditions, the powders, sprays, solutions, lotions and creams available over-the-counter lack effectiveness. The reason for this varies, from poor delivery of the medication to the source or cause of the condition, to loss of the medication through abrasion from normal activity of the patient, to absorption of medications applied to the skin by the patient's socks or clothes. For these various reasons, currently available commercial medications are prone to come off easily once applied to the affected area, and consequently much of the medication is wasted, either through over application in an attempt to anticipate the problem, or in medicine quickly being dispersed away from the site. The medications for these conditions typically require at least 2 to 4 weeks of continuous treatment, and thus often fail due to this poor delivery.

A further problem with the use of existent medications is the lack of compliance by patients. Due to the mess and difficulty of use, patients will often use these over the counter medications only until their symptoms abate and then they will stop the medication, before the recommended course of treatment is completed, and hence often before the infection has truly cleared. Though momentarily abated, the infection then begins to take hold again, and in a matter of days or weeks a full blown infection occurs again. In many cases the patient will repeat using the over the counter medication until the symptoms clear, and again stop the medication with the first sign of abatement, with the whole cycle repeating.

Hence, there is a need for a clean and inexpensive vehicle/carrier of topically applied medications that increases the convenience and effectiveness of the treatment and decreases the necessary time for the treatment. It is preferably associated with less waste and lower cost, and ultimately leads to improved treatment of patient symptoms and increased patient satisfaction.

In medicine, tincture of benzoin and mastic gum (Mastisol) have been employed to form a sticky coating on skin prior to the placement of adhesive preparations. Tincture of benzoin has also been used to form a biologic dressing over superficial cutaneous wounds as well as aphthous ulcers (canker sores). However, the general use of resins, such as mastic and benzoin gum, as semi-permanently applied carriers for increasing the efficacy and usefulness of topological of pharmacological agents has not been disclosed.

A tincture of benzoin has been used with podophyllin resin (10-25%) in the treatment of genital warts. It is considered by many to be cumbersome and inconvenient (see U.S. Pat. Nos. 5,063,065 and 5,167,649). Unfortunately, podophyllin resin is toxic, and even when applied in a tincture of benzoin, this agent must be removed by rigorous washing 1 to 6 hours post-application. Due to the problems associated with using podophyllin resin in tincture of benzoin, other carriers have been sought. As an example, in the treatment of genital warts, Goh, et al. (Singapore Med J (1998) 39:17-19) reports that podophyllin prepared in 0.25% ethanol can be self-applied and is as efficacious as podophyllin prepared in tincture of benzoin and applied in the clinic. Use of tincture of benzoin as a biological bandage with compounds that it is desirable to have in long contact with the skin has not been reported.

Compositions and methods are provided for increasing the effectiveness of treatment of dermatological disorders on the skin or a mucous membrane of a mammal by using a resin or other film-forming agent as a carrier for a pharmacologically active agent. The pharmacological compositions are comprised of one or more resins or other film-forming agents, at least one topically acceptable pharmacologically active agent for treatment of a dermatological disorder other than the resins or other film-forming agents, wherein the active agent is non-toxic to the mammal being treated when left in contact with the lesion of interest for greater than four hours, and a topically acceptable volatile solvent. The compositions optionally can include a penetration enhancer. The methods of treating symptoms of a dermatological disorder include the steps of contacting affected sites on the skin or nails of a patient in need thereof with the pharmacological composition comprised of one or more resins or other film-forming agents, a pharmacological agent or agents, and an evaporative solvent, and allowing it to dry to form a resin-based biological dressing. The biological dressing comprises a sticky film of the one or more resins or other agents which form a film on the skin and a pharmacologically active agent; the latter remains on the skin, nail or mucous membrane after the volatile solvent has evaporated from the one or more resins or other film-forming composition. The dressing forms a hydrophobic, protective film that provides sustained release of the pharmacologically active agent at the site of application. The invention finds use in the treatment of dermatological disorders such as infection, inflammation, and hyperproliferation of epidermal cells.

FIG. 1 is a graphical representation showing data from a skin penetration study of a composition of the invention.

FIG. 2 is a graphical representation showing in vitro franz cell penetration results.

Compositions and methods are provided for the convenient and effective treatment of at least one symptom of a dermatological disorders in a mammal, particularly a human, in need thereof, with a biological dressing. By “biological dressing” or “biologic dressing” or “biologic bandage” is intended a non-occlusive but adherent pharmacological composition that is formed by drying on the skin a pharmacologic composition comprised of one or more resins, such as benzoin, mastic or other compositions that can form a barrier film on the skin, such as compositions that are used as skin wound sealing agents, one or more pharmacologically active agents and a topically acceptable volatile solvent, such as ethanol. The resin-based biologic dressing forms a protective coating at the site(s) on the skin, nails or mucosal membrane exhibiting symptoms of the disorder and also acts as a reservoir for the pharmacologically active agent(s) to provide sustained delivery of an appropriate medication or combination of medications to the site.

The skin disorder symptoms to be treated include, but are not limited to, skin, nail and mucosal membrane lesions, inflammation, itching, scaling and pain. The disorders include viral, fungal and bacterial infections, inflammatory conditions, and hyperproliferative disorders. The pharmacological agent(s) can include topically active agents that can be used to ameliorate skin disorder symptoms, including antimicrobial and antiviral agents, anti-inflammatory agents, analgesics and anesthetics. As desired, the effectiveness of the pharmacological agent(s) optionally can be increased by including a skin or nail penetration enhancer in the pharmacologic composition.

• Provisional Patent
• Utility Patent

• What Is a Patent?
• What Is a Trademark or Servicemark?
• What Is a Copyright?
• Patent Laws