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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