Skin Penetration and Metabolism of Topical Glucocorticoids in Reconstructed Epidermis and in Excised Human Skin

@article{Gysler2004SkinPA,
  title={Skin Penetration and Metabolism of Topical Glucocorticoids in Reconstructed Epidermis and in Excised Human Skin},
  author={Anja Gysler and Burkhard Kleuser and Wolfgang Sippl and Katharina Lange and Hans Christian Korting and Hans-Dieter H{\"o}ltje and Monika Sch{\"a}fer-Korting},
  journal={Pharmaceutical Research},
  year={2004},
  volume={16},
  pages={1386-1391}
}
AbstractPurpose. To investigate pharmacokinetic differences between the non-halogenated double ester prednicarbate (PC) and the fluorinated monoester betamethasone 17-valerate (BM17V) their metabolism in human keratinocytes and fibroblasts as well as their permeation and biotransformation in reconstructed epidermis and excised human skin was compared. Special attention was given to the 17-monoesters because of their high receptor affinity and antiproliferative effects. Methods. Glucocorticoid… 
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83 Citations
Background Citations
18
Methods Citations
5
Results Citations
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83 Citations

Citation Type

Citation Type

Esterase activity in excised and reconstructed human skin--biotransformation of prednicarbate and the model dye fluorescein diacetate.
  • F. M. Bätz, W. Klipper, M. Schäfer-Korting
  • Biology, Medicine
    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
  • 2013
Albumin effects on drug absorption and metabolism in reconstructed epidermis and excised pig skin.
TLDR
Surprisingly, the addition of BSA to the acceptor medium slightly reduced the steroid permeation, especially when formulations of poor PC uptake were tested, and the metabolite pattern changed as compared to PC metabolites to be found in albumin-free acceptormedium.
The impact of skin viability on drug metabolism and permeation -- BSA toxicity on primary keratinocytes.
In vitro skin absorption and drug release - a comparison of six commercial prednicarbate preparations for topical use.
Testosterone Metabolism in Human Skin Cells in vitro and Its Interaction with Estradiol and Dutasteride
TLDR
Dutasteride may be useful in acne and androgenetic alopecia and regulates testosterone action by cell-type-specific activation or deactivation, and effects of 17α-estradiol in androgenetics alopECia are not due to 5α-reductase inhibition.
Drug Targeting by Solid Lipid Nanoparticles for Dermal Use
TLDR
Interestingly, PC incorporation into nanoparticles appeared to induce a localizing effect in the epidermal layer which was pronounced at 6 h and declined later, and may increase the benefit/risk ratio of topical therapy.
The Phenion® Full-Thickness Skin Model for Percutaneous Absorption Testing
TLDR
The Phenion FT model appears to be suitable for percutaneous absorption studies in hazard analysis and should be subjected to a catch-up validation study.
Cyproterone Acetate Loading to Lipid Nanoparticles for Topical Acne Treatment: Particle Characterisation and Skin Uptake
TLDR
Topical CPA treatment of skin diseases should reduce side effects currently excluding the use in males and demanding contraceptive measures in females and may be an additional therapeutic option for acne and other diseases of the pilosebaceous unit.
Ethyl cellulose nanocarriers and nanocrystals differentially deliver dexamethasone into intact, tape-stripped or sodium lauryl sulfate-exposed ex vivo human skin - assessment by intradermal microdialysis and extraction from the different skin layers.
  • N. Döge, S. Hönzke, A. Vogt
  • Biology
    Journal of controlled release : official journal of the Controlled Release Society
  • 2016
Reconstructed Human Epidermis for Skin Absorption Testing: Results of the German Prevalidation Study
TLDR
A protocol based on the OECD principles was developed and prevalidated by using reconstructed human epidermis (RHE) to standardise the predictive testing of percutaneous absorption for regulatory purposes, and the permeation of the OECD standard compounds, caffeine and testosterone, through commercially available RHE models was compared to that of human epidersmis and animal skin.
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References

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TLDR
Based on the results to the in-vivo situation, topically applied PC may be metabolized by epidermal cells during skin penetration, a complex mixture of compounds reaches the dermis, whose fibroblasts are barely able to metabolize the steroids.
Prednicarbate Versus Conventional Topical Glucocorticoids: Pharmacodynamic Characterization In Vitro
TLDR
Correlating antiphlogistic effects in keratinocytes with antiproliferative effects in fibroblasts suggests the improved benefit−risk ratio of PC compared to conventional glucocorticoids does not result only from distinct drug metabolism in the skin but also from a specific influence on the cytokine network.
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TLDR
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TLDR
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TLDR
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TLDR
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