Comparison of the Bioactivity of Mometasone Furoate 0.1% Fatty Cream, Betamethasone Dipropionate 0.05% Cream and Betamethasone Valerate 0.1% Cream in Humans

Bjerring, Peter

doi:10.1159/000211134

Cited by 14 publications

(6 citation statements)

References 10 publications

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“…The introduction of objective bioinstrumental assessments has increased the sensitivity of VCA. Previous works had also advocated the induction of hyperaemia prior to VCA to reveal a more intensive vasoconstriction [14][15][16]. The present findings are at variance with this concept because the blanching effect was best detected when the arm was in the upright position.…”

Section: Discussioncontrasting

confidence: 67%

“…A stronger blanching was then evidenced for corticosteroids only, the peak effect being late (at 6 h) for mometasone furoate and weaker and more delayed (at 24 h) for betamethasone valerate as confirmed by the calculation of the area under the curve. It was not a real surprise as mometasone furoate is a potent corticosteroid [9,15,31,32]. In fact, the peak effect described here does not correspond to a maximum blanching that could occur a couple of hours before or after the predetermined assessment times.…”

Section: Discussionmentioning

confidence: 70%

“…The sensitivity of these instrumental methods was not always adequate to discriminate the activity of distinct corticosteroids. Hence, VCA was sometimes performed after stripping or after induction of vasodilation either by ultraviolet light [14,15] or ischaemia [16] in normal volunteers. Patients suffering from essential hypertension also showed increased vasoconstrictor sensitivity to corticosteroids [17].…”

Section: Introductionmentioning

confidence: 99%

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Postural Skin Colour Changes during the Corticosteroid Blanching Assay

Henry¹,

Fumal²,

Piérard³

1999

Skin Pharmacol Physiol

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Objective: To assess the effect of the position of a limb (dependency) on the cutaneous vasoconstrictor (blanching) assay (VCA) using topical corticosteroid preparations. Method: Two studies were performed on the forearms of healthy volunteers using tristimulus reflectance colorimetric assessments. The first one conducted in 60 normal adults aimed at quantifying the range of variation in the skin chromaticity a* when the arm was successively positioned horizontally and vertically, either in the upward or downward direction. In the second study, 16 volunteers were selected according to a weak spontaneous postural dependency of the limb in a* (<2 units). The blanching effect of 0.1% mometasone furoate, 0.1% betamethasone valerate and petrolatum were compared to the colour of an untreated site. Chromaticity a* and the colorimetric variable (ΔtL*² + Δta*²)^0.5 were measured in time following a 2-hour application. Results: The postural variations in skin colour varied among subjects. The majority of them (80%) presented a difference in a* higher than 2 units between the upright and downward arm positions. The upright position appeared to be the most sensitive to show significant differences in the VCA. Mometasone furoate exhibited the most prominent effect, significantly higher than betamethasone valerate and controls. Conclusion: The corticosteroid VCA is influenced by the position of the limb. The upright position increases the sensitivity of the test. Mometasone furoate is more potent than betamethasone valerate.

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Section: Discussioncontrasting

confidence: 67%

Section: Discussionmentioning

confidence: 70%

Section: Introductionmentioning

confidence: 99%

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Postural Skin Colour Changes during the Corticosteroid Blanching Assay

Henry¹,

Fumal²,

Piérard³

1999

Skin Pharmacol Physiol

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“…44 These properties might contribute to the in vivo protective effect of the JW-E against UV light-induced skin inflammation; in fact, lipid peroxidation products exert acute inflammatory effects in mammalian skin, 45 and several papers support the usefulness of the UVB erythema test for evaluation of steroidal and non-steroidal antiinflammatory agents. 46,47 In conclusion, the present in vitro and in vivo findings demonstrate that the JW-E possesses a strong antioxidant/free radical-scavenging effectiveness, which is very likely due to the phenolic compounds contained in it. Furthermore, this extract gives excellent photoprotection against UVB-induced skin damage; thus its use could have important therapeutic applications in certain skin diseases caused, initiated or exacerbated by ROS and free radical overproduction.…”

Section: Resultsmentioning

confidence: 60%

Chemical analysis and photoprotective effect of an extract of wine from Jacquez grapes

et al. 2002

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The present study was aimed at evaluating the in vitro antioxidant activity and in vivo photoprotective activity of an extract of wine obtained from Jacquez (Vitis aestivalis-cinerea Â V vinifera) grapes (JW-E). The chemical profile of the JW-E was characterised by a significant level of proanthocyanidins, together with lower amounts of anthocyanins and hydroxycinnamic acids. The antioxidant activity of the JW-E was assessed by means of various in vitro tests (bleaching of the stable 1,1-diphenyl-2-picrylhydrazyl radical; peroxidation, induced by the water-soluble radical initiator 2,2'-azobis(2-amidinopropane) hydrochloride, on mixed dipalmitoylphosphatidylcholine/linoleic acid unilamellar vesicles; UV radiation-induced peroxidation in phosphatidylcholine multilamellar vesicles). In all in vitro tests employed, the JW-E proved to possess strong antioxidant/free radicalscavenging effectiveness. Furthermore, when topically applied, a gel formulation containing the JW-E afforded significant in vivo protection against UVB light-induced skin erythema (monitored by reflectance spectrophotometry) in healthy human volunteers.

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“…Therefore, DCE appears disappointing from the therapeutical point of view, but scientifically speaking, DCE might respresent an 'opposite PC', with remarkable activities in fibroblasts and negligible influences on keratinocytes. This, however, does not apply to halogenated monoesters in general, as mometasone 17-furoate [22][23][24] is reported to be well tolerated. This drug, however, has been tested less extensively as compared to PC.…”

Section: Discussionmentioning

confidence: 99%

Cutaneous Inflammation and Proliferation in vitro: Differential Effects and Mode of Action of Topical Glucocorticoids

Lange

Kleuser

Gysler

et al. 2000

Skin Pharmacol Physiol

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The nonhalogenated double ester of prednisolone, prednicarbate (PC), is the first topical glucocorticoid with an improved benefit/risk ratio verified clinically and in vitro. To evaluate if this is due to unique characteristics of this steroid, a new compound created according to an identical concept, prednisolone 17-ethylcarbonate, 21-phenylacetate (PEP), and the new halogenated monoester desoximetasone 21-cinnamate (DCE) were tested and compared to PC, desoximetasone (DM) and betamethasone 17-valerate (BMV). Isolated foreskin keratinocytes served for in vitro investigations of anti-inflammatory processes in the epidermis, fibroblasts of the same origin were used to investigate the atrophogenic potential. Inflammation was induced by TNFα, resulting in an increased interleukin 1α (Il-1α) synthesis. As quantified by ELISA, all drugs significantly reduced Il-1α production. But PC and BMV appeared particularly potent, followed by DM and the two new congeners, which revealed minor anti-inflammatory activity. Glucocorticoid esters including PEP are rapidly degraded in keratinocytes (85% within 12 h). Hence, a ribonuclease protection assay of Il-1α mRNA was performed allowing short incubation times and thus minimizing biodegradation. This assay confirmed the anti-inflammatory potency of native PC and BMV. In contrary DCE and PEP did not reduce Il-1α mRNA to a significant extent. Therefore PEP acts as a prodrug only. In fibroblasts, Il-1α and Il-6 syntheses indicate proliferation and inflammation, respectively. Whereas PC and PEP inhibited Il-1α and Il-6 production in fibroblasts only to a minor extent, cytokine synthesis was strongly affected by the conventional glucocorticoids BMV and DM, but also by DCE. The minor unwanted effect of PC and PEP on fibroblasts was also reflected by their low influence on cell proliferation as derived from ³H-thymidine incorporation. Again, more pronounced antiproliferative features were seen with the halogenated glucocorticoids. In the following, the correlation between antiphlogistic effects in keratinocytes (suppression of Il-1α) and antiproliferative effects in fibroblasts (suppression of Il-1α and Il-6; ³H-thymidine incorporation) was analyzed. Here, PC is revealed as the only glucocorticoid with an improved benefit/risk ratio. Native PEP is shown to be almost ineffective and DCE presents exactly the opposite features of PC. It is tempting to speculate if this is due to different glucocorticoid receptor subtypes or different signaling pathways in keratinocytes and fibroblasts.

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Comparison of the Bioactivity of Mometasone Furoate 0.1% Fatty Cream, Betamethasone Dipropionate 0.05% Cream and Betamethasone Valerate 0.1% Cream in Humans

Cited by 14 publications

References 10 publications

Postural Skin Colour Changes during the Corticosteroid Blanching Assay

Postural Skin Colour Changes during the Corticosteroid Blanching Assay

Chemical analysis and photoprotective effect of an extract of wine from Jacquez grapes

Cutaneous Inflammation and Proliferation in vitro: Differential Effects and Mode of Action of Topical Glucocorticoids

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