Activity of Different Desoximetasone Preparations Compared to Other Topical Corticosteroids in the Vasoconstriction Assay

Borelli, Claudia; Gassmueller, J.; Fluhr, Joachim W.; Nietsch, K. H.; Schinzel, S.; Körting, Hans Christian

doi:10.1159/000131082

Cited by 6 publications

(4 citation statements)

References 17 publications

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“…Desoximetasone is a synthetic topical corticosteroid used to treat mild to moderate psoriasis effectively. Desoximetasone has been used in various semisolid dosage forms such as creams, ointments, and gels; however, all of these formulations are limited in terms of controlled release applications, since no product with sustained release is currently commercially available [ 27 , 28 , 29 ].…”

Section: Introductionmentioning

confidence: 99%

Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

Shah

Goodyear

Dholaria

et al. 2021

IJMS

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Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.

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Section: Introductionmentioning

confidence: 99%

Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

Shah

Goodyear

Dholaria

et al. 2021

IJMS

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“…It is based on the property of corticosteroids to induce vasoconstriction represented by blanching of the skin [19][20][21] . The vasoconstrictive strength is known to correlate strongly with the clinical efficacy of topical glucocorticoids as determined in clinical treatment trials [22] .…”

Section: Introductionmentioning

confidence: 99%

Bioavailability, Antipsoriatic Efficacy and Tolerability of a New Light Cream with Mometasone Furoate 0.1%

Körting

Schöllmann

Willers

et al. 2012

Skin Pharmacol Physiol

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Mometasone furoate, a potent glucocorticoid (class III) with a favorable benefit/risk ratio, has emerged as a standard medication for the treatment of inflammatory skin disorders. The purpose of the investigation presented here was to determine the noninferiority of a topical mometasone formulation, a light cream (O/W 60/40 emulsion) with mometasone furoate 0.1% (water content of 33%) versus marketed comparators. Using the vasoconstrictor assay, a strong blanching effect of the new cream (called Mometasone cream) comparable to that of a mometasone comparator, a fatty cream with mometasone furoate 0.1%, could be demonstrated. Thus, the topical bioavailability of the active ingredient mometasone furoate (0.1%) was regarded to be similar for Mometasone cream and the mometasone comparator. Using the psoriasis plaque test, a strong antipsoriatic effect comparable to that of the mometasone comparator was found for Mometasone cream after 12 days of occlusive treatment. A nearly identical reduction in the mean infiltrate thickness and similar mean AUC values were noted with both formulations confirmed by clinical assessment data. The noninferiority of Mometasone cream to its active comparator with respect to the AUC of change to baseline in infiltrate thickness was demonstrated. Both medications were well tolerated. Overall, Mometasone cream and the mometasone comparator showed similar efficacy and tolerability. Mometasone cream, in addition to its high potency and good tolerability, provides the properties of a light cream, which might make this new medication particularly suitable for application on acutely inflamed and sensitive skin.

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“…A first approach to the development of an in vitro test system was based on the inhibition of interleukin (IL)-1 synthesis in normal human keratinocytes and fibroblasts (13). The results were in close correlation with those from studies in human volunteers, when comparing GCs which varied in safety but were similar in skin blanching (16). The latter effect is used for the estimation of clinical potency (17).…”

Section: Introductionmentioning

confidence: 79%

Evaluation of Anti-inflammatory and Atrophogenic Effects of Glucocorticoids on Reconstructed Human Skin

2011

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Topical glucocorticoids (GCs) are extensively used in the treatment of inflammatory skin diseases. However, their long-term use is often accompanied by severe and eventually irreversible adverse effects, with atrophy being the most important limitation. Currently, most non-clinical studies involve animal testing, so the results are not always representative of the situation in humans. The aim of this project was to establish an in vitro test protocol for the evaluation of the anti-inflammatory and atrophic potential of topically applied GCs in reconstructed human skin. Initial studies with fibroblasts and keratinocytes confirmed the anti-inflammatory and atrophogenic effects of GCs, as evidenced by decreased cytokine production and collagen mRNA expression. In non-pretreated reconstructed human skin (EpiDermFT™), the topical application of GCs for seven days strongly reduced the secretion of interleukin (IL)-6. GC-induced skin atrophy, known to appear only after prolonged treatment, was not detected by the analysis of epidermal thickness and collagen mRNA expression. However, reproducible epidermal inflammation was established for the first time in reconstructed human skin. Topical treatment with tumour necrosis factor (TNF) increased IL-6 release and strongly reduced epidermal thickness accompanied by severe parakeratosis. GC treatment of reconstructed human skin reduced IL-6 levels and completely resolved parakeratosis, leading to the normalisation of epidermal thickness. These induced inflammatory conditions mimic more closely the clinical situations in which GCs are used, and therefore appear to be more suitable for future investigations for the establishment of a human-based in vitro test protocol for evaluating wanted and unwanted GC effects.

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Activity of Different Desoximetasone Preparations Compared to Other Topical Corticosteroids in the Vasoconstriction Assay

Cited by 6 publications

References 17 publications

Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

Bioavailability, Antipsoriatic Efficacy and Tolerability of a New Light Cream with Mometasone Furoate 0.1%

Evaluation of Anti-inflammatory and Atrophogenic Effects of Glucocorticoids on Reconstructed Human Skin

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