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Soft Silicone Elastomer Emulsion as topical drug delivery system

IP.com Disclosure Number: IPCOM000235035D
Publication Date: 2014-Feb-25
Document File: 8 page(s) / 49K

Publishing Venue

The IP.com Prior Art Database

Abstract

Disclosed are formulation possibilities for dermatological treatments with a technology based on emulsion from soft silicone elastomer stabilized by a film former such as but not limited to a polyvinyl alcohol (PVA). When applied on an artificial substrate or on the skin, the film formed is a dual film made of a soft elastomer covered by a top layer of polyvinyl alcohol. Depending on the various ratios of silicone elastomer to polyvinyl alcohol, a broad variety of films can be obtained. This composition latitude can deliver a range of films covering a broad appearance spectrum from glossy to matte, white to transparent and varying mechanical properties. Disclosed are drug loaded formulation possibilities of this technology with both a hydrophilic model drug (caffeine, logP = -0.07) and lipophilic model drug (betamethasone dipropionate or BDP, logP = 4.23) capable of delivering the drug substance. Their performance testing demonstrated the diffusion of the drug substance through the stratum corneum. Such drug loaded formulations of this technology can be particularly useful in topical applications.

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Soft Silicone Elastomer Emulsion as topical drug delivery system

Authors: Morgane Le Meur1, Séverine Cauvin1, Laurie Maes1, Anick Colson1, Stéphane Cornelis1, Xavier Thomas2

                                                                                               1 Dow Corning Europe S.A.

                                                                                               2 Dow Corning France S.A.S.

Abstract

Disclosed are formulation possibilities for dermatological treatments with a technology based on emulsion from soft silicone elastomer stabilized by a film former such as but not limited to a polyvinyl alcohol (PVA). When applied on an artificial substrate or on the skin, the film formed is a dual film made of a soft elastomer covered by a top layer of polyvinyl alcohol. Depending on the various ratios of silicone elastomer to polyvinyl alcohol, a broad variety of films can be obtained. This composition latitude can deliver a range of films covering a broad appearance spectrum from glossy to matte, white to transparent and varying mechanical properties.

Disclosed are drug loaded formulation possibilities of this technology with both a hydrophilic model drug (caffeine, logP = -0.07) and lipophilic model drug (betamethasone dipropionate or BDP, logP = 4.23) capable of delivering the drug substance. Their performance testing demonstrated the diffusion of the drug substance through the stratum corneum. Such drug loaded formulations of this technology can be particularly useful in topical applications.

       I.            Background

An alkenyl-containing organopolysiloxane having an average per molecule of at least 2 alkenyl groups and an SiH containing siloxane having an average per molecule of at least 2 SiH moieties are emulsified with an aqueous polyvinyl alcohol (PVA) solution. A non-polymeric surfactant is optionally added. Reaction of the alkenyl-containing organopolysiloxane and SiH containing siloxane occurs thanks to the addition of a hydrosilylation catalyst which is added to the emulsion simultaneously with the aqueous PVA or which is added to the aqueous silicone emulsion subsequently. Silicone elastomer droplets of dimethicone crosspolymer are thus formed in situ. When applied on a substrate such as skin by means such as coating brushing or spraying, and after drying at room temperature or under warm condition, a film is formed.

    II.            Materials

1.      Silicone emulsion preparation

The soft silicone elastomer emulsion technology also called Silicone PVA Emulsion technology allows a broad range of films that can be very different depending on the silicone elastomer and polyvinyl alcohol ratios. When applied on an artificial substrate or on the skin, the film formed is a dual film made of a soft silicone elastomer covered by a top layer of polyvinyl alco...