Topical composition comprising a film-forming polymer for delivering an active ingredient to skin

Abstract

A film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a volatile solvent, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent. The composition is capable of forming, after application on skin and evaporation of the solvent, a continuous phase comprising the film-forming polymer and the plasticizer and a dispersed phase comprising droplets of the oily release-enhancing agent.

Description

FIELD OF INVENTION[0001]The present invention relates to a pharmaceutical composition for application on skin and containing a film-forming polymer and at least one active ingredient, the composition forming a thin and transparent two-phase film on the skin on evaporation of a solvent.BACKGROUND OF THE INVENTION[0002]Human skin, in particular the outer layer, the stratum corneum, provides an effective barrier against penetration of microbial pathogens and toxic chemicals. While this property of skin is generally beneficial, it complicates the dermal administration of pharmaceuticals in that a large quantity, if not most, of an active ingredient applied on the skin of a patient suffering from a dermal disease may not penetrate into the viable layers of the skin where it exerts its activity. To ensure an adequate penetration of the active ingredient into the dermis and epidermis, it is generally preferred to include the active ingredient in a dissolved state, typically in the presence...

AI Technical Summary

Benefits of technology

[0016]In the course of research leading to the invention, it was surprisingly found that the oily release-enhancing agent forms oil droplets in the film upon evaporation of the solvent (cf. Example 8 and 9 showing results of atomic force microscopy (AFM) measurements of film-forming compositions disclosed herein). Without being limited to any particular theory, it is assumed that the increased release obtained from film-forming compositions comprising an oily release-enhancing agent may be the result of diffusion of the active ingredient from the matrix of film-forming polymer and plasticizer into the oil droplets from which the active ingredient is released resulting in increased and continuous release from the film-forming composition. Furthermore, the oily release-enhancing agent may act as an emollient to improve hydration of the skin and control transepidermal water loss, thus reinforcing the occlusive effect of the film-forming polymer.

Problems solved by technology

Film-forming compositions disclosed in the literature suffer from the drawback that only a minor proportion of the active ingredient incorporated therein is released from the composition.

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