Idea Ag

Tdt Limited

Sequessome Technology Holdings Limited

Ulrich Vierl

Gregor Cevc

John Charles Mayo

George Langton Iliffe

Matthias Rother

The present invention relates to topical antifungal formulations terbinafine or a pharmaceutically acceptable salt thereof, a lipid, and a surfactant, and uses thereof for the treatment of skin and nail fungal infections.

Topical terbinafine formulations and methods of administering same for the treatment of fungal infections

The invention describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDs) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID from a solution on the skin surface. This is believed to be due to the special ability of suitable large carriers to bypass the local sink of blood capillaries at the epidermal-dermal junction in the skin. The carrier-mediated delivery of locally applied NSAIDs thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.

NSAID formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery

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Groebenzell, Germany

Ulrich Vierl