Prednicarbate Versus Conventional Topical Glucocorticoids: Pharmacodynamic Characterization In Vitro

@article{Lange2004PrednicarbateVC,
  title={Prednicarbate Versus Conventional Topical Glucocorticoids: Pharmacodynamic Characterization In Vitro},
  author={Katharina Lange and Anja Gysler and Michael Bader and Burkhard Kleuser and Hans Christian Korting and Monika Sch{\"a}fer-Korting},
  journal={Pharmaceutical Research},
  year={2004},
  volume={14},
  pages={1744-1749}
}
AbstractPurpose. Pharmacodynamic characterization of topical glucocorticoids as prednicarbate (PC), its metabolites prednisolone 17-ethylcarbonate (PEC) and prednisolone (PD), betamethasone 17-valerate (BMV), beta-methasone (BM) and desoximetasone (DM) by evaluating their effects on epidermal and dermal cells. Synopsis of pharmacokinetic and pharmacodynamic studies, possibly explaining the improved benefit-risk ratio of prednicarbate. Methods. Isolated foreskin keratinocytes were used to… 
Skin Penetration and Metabolism of Topical Glucocorticoids in Reconstructed Epidermis and in Excised Human Skin
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In vitro determination of the dermal 17-monoesters concentrations may allow the prediction of the atrophogenic risk in man and the inactivation of highly potent, but also cell toxic, 17- monoesters to almost inactive 21-congeners appears less important in the skin.
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TLDR
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TLDR
A new approach to in vitro quantification of the benefit-risk ratio has been developed, and drugs that selectively modulate cytokine release appear to be equipotent alternatives to the gold standard betamethasone 17-valerate with respect to anti-inflammatory activity.
Prednicarbate (Dermatop®): Profile of a Corticosteroid
TLDR
Prednicarbate is a nonhalogenated, double-ester derivative of prednisolone that has been used in the treatment of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses such as atopic dermatitis and has a favorable benefit–risk ratio, low skin atrophy potential, and high anti-inflammatory action.
Prednicarbate (Dermatop®): Profile of a Corticosteroid
TLDR
Prednicarbate is a nonhalogenated, double-ester derivative of prednisolone that has been used in the treatment of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses such as atopic dermatitis and has a favorable benefit–risk ratio, low skin atrophy potential, and high anti-inflammatory action.
New and Established Topical Corticosteroids in Dermatology
TLDR
The new molecules, compared with the well known and established corticosteroids, generally have a higher anti-inflammatory effect, good compliance among patients (only a once-daily application is needed), rarely induce cross-sensitivity reactions and have weak atrophogenicity.
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.
Investigations of in vitro test systems for the detection of Glucocorticoid-induced skin atrophy as a tool in drug discovery
TLDR
A cascade of three in vitro models based on NHEK, 3T3 fibroblasts and FTSM is recommended to be applied for the characterization of the atrophogenicity of GC receptor ligands and the predictability of these models for the clinical situation is analyzed.
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