Dependence of corticosteroid penetration on the vehicle

Polano, M. K.

doi:10.1001/archderm.112.5.675

Cited by 28 publications

(19 citation statements)

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“…Also the composition of the vehicle has a substantial influence on the potency of topical preparations [14][15][16], Since the introduction of corticosteroids, chemical engineering has provided a series of optimized steroid molecules for topical prep arations [16,20], Mometasone furoate is a recently introduced synthetic corticosteroid in which the steroid nucleus is a 16-methyl analogue of beclomethasone with a 21 -chloro group and a novel (2') furoate 17-ester. Mom etasone furoate is strongly lipophilic, which seems to be associated with a high penetration rate [20].…”

Section: Discussionmentioning

confidence: 99%

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

Bjerring¹

1993

Skin Pharmacol Physiol

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The bioactivity of a novel topical glucocorticosteroid, mometasone furoate 0.1 % fatty cream was compared with betamethasone dipropionate 0.05% cream and betametasone valerate 0.1% cream. An ultraviolet light (UV-B)-induced inflammation assay in humans was used, and the combined effect of a single, open application of the corticosteroids was evaluated. Reduction of UV-B induced inflammation was monitored by laser Doppler blood flowmetry, clinical skin scoring and skin reflectance spectrophotometry. Skin scoring and reflectance spectrophotometry were found unsuitable because one of the cream vehicles contained titanium dioxide which shielded skin erythema. Laser Doppler blood flowmetry showed that mometasone furoate 0.1 % fatty cream was more than twofold better in reducing UV-B-induced inflammation than betamethasone dipropionate 0.05% cream and betametasone valerate 0.1 % cream, and that the effect was sustained for at least 24 h after a single application.

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Section: Discussionmentioning

confidence: 99%

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

Bjerring¹

1993

Skin Pharmacol Physiol

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“…PG and PEG which are commonly used solvents in the pharmaceutical industries were employed in this study as permeation enhancers. Previous studies have postulated that PG may carry the drug through the barrier layer (28,29) while other studies describe that PG as a hydrophilic material enters the keratin in the corneocyte but does not alter the lipid fluidity in hydrated tissue (30). More recently, it has been suggested that PG as a hydrophilic material with two hydroxyl group could replace water at the binding sites in the polar head group region and may act in a similar way to water (31).…”

Section: Tablementioning

confidence: 99%

Applying response surface methodology to optimize nimesulide permeation from topical formulation

Shahzad¹,

Afreen²,

Shah³

et al. 2012

Pharmaceutical Development and Technology

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Nimesulide is a non-steroidal anti-inflammatory drug that acts through selective inhibition of COX-2 enzyme. Poor bioavailability of this drug may leads to local toxicity at the site of aggregation and hinders reaching desired therapeutic effects. This study aimed at formulating and optimizing topically applied lotions of nimesulide using an experimental design approach, namely response surface methodology. The formulated lotions were evaluated for pH, viscosity, spreadability, homogeneity and in vitro permeation studies through rabbit skin using Franz diffusion cells. Data were fitted to linear, quadratic and cubic models and best fit model was selected to investigate the influence of permeation enhancers, namely propylene glycol and polyethylene glycol on percutaneous absorption of nimesulide from lotion formulations. The best fit quadratic model explained that the enhancer combination at equal levels significantly increased the flux and permeability coefficient. The model was validated by comparing the permeation profile of optimized formulations' predicted and experimental response values, thus, endorsing the prognostic ability of response surface methodology.

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“…Zinc oxide is one of the essential com ponents of Lassar's paste, the classical base for dithranol therapy [3], However, in other vehicles, such as paraffin, vaseline or creams, the preservative effect of salicylic acid has never been proven [4,5]. An en hancement of the penetration of other phar-maca has been demonstrated with salicylic acid in concentrations of 10% or more [6], Up to now such an effect has never been shown for the lower concentrations of sali cylic acid.…”

Section: Introductionmentioning

confidence: 99%

The Relevance of Salicylic Acid in the Treatment of Plaque Psoriasis with Dithranol Creams

Mare

Calis

Hartog

et al. 1988

Skin Pharmacol Physiol

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The relevance of salicylic acid in dithranol creams was evaluated in a double-blind study. Patients with chronic plaque psoriasis were treated using a short-contact schedule for dithranol on an outpatient basis. A left-right comparison was carried out between sites treated with either dithranol with 2 % salicylic acid (D+S) or dithranol in the same base without salicylic acid (D-S). Clinical results were evaluated once a week using the psoriasis area severity index. In order to quantify the improvement, flow cytometric measurements were done using the monoclonal antibody K_s8.12, recognizing keratin 16 in normal and lesional epidermis. Simultaneously, relative DNA content was quantified which previously was described as a useful method to monitor a therapeutic effect. Both PASI scores and K_s8.12 binding decreased after 6 weeks treatment with D+S and D-S. However, percentages of cells in SG₂M phases did not show a significant change. No significant difference was observed between sites treated with either D+S or D-S. Therefore we conclude that the addition of salicylic acid in a concentration of 2 % does not enhance the efficacy of dithranol creams and we confirm that K_s8.12 is a useful quantitative marker for therapeutic efficacy.

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Dependence of corticosteroid penetration on the vehicle

Cited by 28 publications

References 0 publications

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

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

Applying response surface methodology to optimize nimesulide permeation from topical formulation

The Relevance of Salicylic Acid in the Treatment of Plaque Psoriasis with Dithranol Creams

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