GD - Online U. Münster et al.: Antidrogen targeting to the hair follicle
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U. Münster (1), K. Jores (2), W. Mehnert (2), M. Schaller (3), H.C. Korting (3) and M. Schäfer Korting (1)

Antidrogen targeting to the hair follicle

Depts. of Pharmacy (1) Pharmacology, (2) Pharmaceutical Technology)
Freie Universität D 14195 Berlin
( 3) Dermatology, Ludwig MaximiliansUniversität, D 80337 München

Acne vulgaris and androgenetic alopecia are linked to endogenous androgen production. In man systemic side effects exclude even topical treatment by androgen receptor antagonists. This, however, may become possible by antiandrogen targeting to the hair follicle. Here we present the Penetration Profile of a new potent antiandrogen RU 58841 into porcine skin comparing various vehicles including drug carrier systems. Penetration studies were carried out using the Franz diffusion cell. After 6 h incubation excessive material was removed and the skin was Tesa stripped and cut into 100pm slices. Dried extracts of the slices and Tesa strips were analysed by HPLC. Moreover, RU 58841 metabolism in cultured human foreskin keratinocytes and fibroblasts was investigated. When applied as an ethanolic solution (50p1) up to 3 % of the applied drug penetrated the tissue and 53 to 77 % of the penetrated substance was recovered by tesa stripping. RU 58841 penetration decreased in the following order . ethanolic solution > "Elektrodengel DAS" > "nichtionische hydrophile Creme NRF". RU 58841 was not metabolised in any of the porcine skin sampies nor in human foreskin keratinocytes and fibroblasts. To demonstrate drug targeting to the hair follicle silver labelled solid lipid nanoparticles (SLN) were applied to porcine skin, too. Intact silver labelled SLN were detectable in deeper layers of the hair follicle. Therefore the association of antiandrogens with SLN may allow for topical therapy of acne and androgenetic alopecia not only in women but also in men.

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