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Bodenlenz, M; Dragatin, C; Liebenberger, L; Tschapeller, B; Boulgaropoulos, B; Augustin, T; Raml, R; Gatschelhofer, C; Wagner, N; Benkali, K; Rony, F; Pieber, T; Sinner, F.
Kinetics of Clobetasol-17-Propionate in Psoriatic Lesional and Non-Lesional Skin Assessed by Dermal Open Flow Microperfusion with Time and Space Resolution.
Pharm Res. 2016; 33(9):2229-2238
Doi: 10.1007/s11095-016-1960-y
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- Leading authors Med Uni Graz
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Sinner Frank Michael
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Weiss Manfred
- Co-authors Med Uni Graz
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Boulgaropoulos Beate
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Gatschelhofer Christina
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Pieber Thomas
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- Abstract:
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To evaluate the kinetics of topically applied clobetasol-17-propionate (CP-17) in lesional and non-lesional psoriatic skin when released from a commercially available low-strength cream using in vivo dermal open-flow microperfusion (dOFM).
Twelve patients received Dermovate® cream (CP-17, 0.05%) on small lesional and non-lesional skin test sites for 14 days, once daily. On day 1 and 14, dOFM samples were continuously taken in the dermis for 24 h post-dose and analyzed by LC-MS/MS. Probe depths were assessed by 50 MHz ultrasound scanning.
Mixed-effects modelling identified skin condition, treatment duration and probe-depth as kinetics determining variables. The time- and depth-resolved intradermal data revealed (i) slower penetration of CP-17 into lesional than into non-lesional skin, (ii) normalized (faster) skin penetration after repeated dosing, and (iii) no CP-17 accumulation within the dermis independently of the skin condition.
Intradermal investigation of a highly lipophilic drug released from low-strength cream was successfully performed by using dOFM and timely and spatially, i.e., probe-depth dependent, resolved kinetic data were delivered. These data support the assumption that the thickened psoriatic stratum corneum might act as trap compartment which lowers the skin penetration rate for lipophilic topical drugs.
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Administration, Cutaneous -
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Adult -
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Chromatography, Liquid - methods
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Clobetasol - administration & dosage
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Clobetasol - pharmacokinetics
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Female -
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Humans -
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Kinetics -
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Male -
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Perfusion - methods
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Skin - drug effects
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Skin - metabolism
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Skin Absorption - physiology
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Tandem Mass Spectrometry - methods
- Find related publications in this database (Keywords)
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dermal pharmacokinetics
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lipophilic drug
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open flow microperfusion
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skin penetration
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topical formulation