Topical corticosteroids in psoriasis: strategies for improving safety

Horn, EJ; Domm, Silja; Katz, H. Irving; Lebwohl, Mark; Mrowietz, Ulrich; Kragballe, Knud

doi:10.1111/j.1468-3083.2009.03358.x

Cited by 65 publications

(52 citation statements)

References 41 publications

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“…Their clinical efficacy is associated with drug skin retention; however, they can permeate the stratum corneum, reaching deeper skin layers, which may cause local and systemic side effects (Zhang, Smith, 2011). Clobetasol propionate (CP) is a superpotent topical corticosteroid (USA class I as per Stoughton-Cornell classification) (Horn et al, 2010). Skin atrophy, skin infections, and hypothalamic-pituitary-adrenal (HPA) axis suppression are some of the possible side effects of topical corticosteroids, which are related to the clinical potency of the drug (Horn et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

Silva

Taveira

Lima

et al. 2012

Braz. J. Pharm. Sci.

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Clobetasol propionate (CP) is a potent topical corticosteroid that causes several cutaneous and systemic side effects. In the present work, CP was encapsulated in nanostructured lipid carriers (NLCs) to increase drug retention in the outer skin layers and improve the safety of topical therapy. NLCs were prepared using a microemulsion technique with a mixture of lecithin, taurodeoxycholate, stearic acid, and oleic acid. In vitro penetration studies were performed in a modified Franz-type diffusion cell, and porcine ears were used as a model of human skin. A simple and sensitive liquid chromatographic method was developed and validated for clobetasol determination in different skin layers. NLCs presented uniform size distribution, high zeta potentialand entrapment efficiency values (> 98%). The analytical procedure was validated according to FDA guidelines. Clobetasol recoveries from skin samples were higher than 85%, with no interference of skin components and NLC ingredients. In experiments, after 6 h, a higher drug accumulation in the stratum corneum arising from NLCs compared to aqueous CP solution was observed. Thus, the NLCs demonstrated high potential for targeting CP to the skin and ensuring drug accumulation in the stratum corneum.Uniterms: Clobetasol propionate/in vitro skin penetration. Nanostructured lipid carriers/in vitro study.Proprionato de clobetasol (CP) é um potente corticóide tópico, que apresenta vários efeitos adversos cutâneos e sistêmicos. No presente trabalho, CP foi encapsulado em carreadores lipídicos nanoestruturados (NLCs) visando aumentar a retenção do fármaco nas camadas superficiais da pele e a segurança da terapia tópica. NLCs foram preparados usando a técnica de diluição de microemulsão com mistura de lecitina, taurodesoxicolato, ácido esteárico e ácido oléico. Estudos de penetração in vitro foram realizados em células de difusão de Franz modificadas usando pele de orelha de porco como modelo de pele humana. Um método simples e sensível de cromatografia líquida foi desenvolvido e validado para a determinação de clobetasol nas diferentes camadas da pele. NLCs apresentaram distribuição de tamanho uniforme e valores elevados de potencial zeta e eficiência de encapsulação (>98%). O procedimento analítico foi validado de acordo com as diretrizes do FDA. A recuperação de clobetasol a partir das amostras de pele foi maior que 85%, sem interferência dos componentes da pele e dos excipientes das NLCs. Após 6 horas de experimento observou-se maior acúmulo do fármaco a partir das NLCs comparado à solução aquosa de CP. Dessa forma, as NLCs mostraram elevado potencial para direcionar o CP para a pele, pois elas possibilitaram o acúmulo do fármaco no estrato córneo. Unitermos: Proprionato de clobetasol/penetração cutânea in vitro. Carreadores lipídicos nanoestruturados/ estudo in vitro.

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Section: Introductionmentioning

confidence: 99%

In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

Silva

Taveira

Lima

et al. 2012

Braz. J. Pharm. Sci.

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“…However depending on its potency, many side effects are observed with respect to the other members of the steroid drugs. 19 Effectiveness of topical corticosteroids is related to their vasoconstrictive, anti-inflammatory, immunosuppressive, and antiproliferative effects in the treatment of psoriasis and atopic dermatitis. 20,21 The skin blanching assay has been used in many studies depending on the direct correlation between corticosteroid-induced skin blanching and vasoconstriction.…”

Section: Introductionmentioning

confidence: 99%

Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Özcan¹,

Azizoğlu²,

Şenyiğit³

et al. 2013

IJN

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Abstract:The objective of this study was to prepare a suitable formulation for dermal delivery of diflucortolone valerate (DFV) that would maintain the localization in skin layers without any penetration and to optimize efficiency of DFV. Drug-loaded lecithin/chitosan nanoparticles with high entrapment efficiency (86.8%), were successfully prepared by ionic interaction technique. Sustained release of DFV was achieved without any initial burst release. Nanoparticles were also incorporated into chitosan gel at different ratios for preparing a more suitable formulation for topical drug delivery with adequate viscosity. In ex-vivo permeation studies, nanoparticles increased the accumulation of DFV especially in the stratum corneum + epidermis of rat skin without any significant permeation. Retention of DFV from nanoparticle in chitosan gel formulation (0.01%) was twofold higher than commercial cream, although it contained ten times less DFV. Nanoparticles in gel formulations produced significantly higher edema inhibition in rats compared with commercial cream in in-vivo studies. Skin blanching assay using a chromameter showed vasoconstriction similar to that of the commercial product. There were no barrier function changes upon application of nanoparticles. In-vitro and in-vivo results demonstrated that lecithin/chitosan nanoparticles in chitosan gel may be a promising carrier for dermal delivery of DFV in various skin disorders.

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“…Some steroids which are widely used in topical psoriasis treatment but have not been discussed in this section include, methylprednisolone aceponate (Ruzicka 2006), which has shown good efficacy against chronic therapy-resistant psoriasis, including both progressive and stationary phases. Although topical corticosteroids are effective in maintenance of the disease, these therapies can cause many potential local adverse effects including cutaneous atrophy, formation of telangiectasia, development of striae, steroid rosacea, perioral dermatitis, and skin infections (Horn et al, 2010). Risks of systemic adverse effects increase with prolonged use, or use of higher potency steroids, particularly with greater percent of BSA to which the topical steroid drug is applied.…”

Section: Corticosteroidsmentioning

confidence: 99%

“…Topical corticosteroids are often classified into seven classes in United States and four in UK and Germany based on potency. A detailed classification system has been discussed else where (Horn et al, 2010). In the United States, topical corticosteroids are classified as following: class I (superpotent), class II (potent), class III (upper mid strength), class IV (mid strength), class V (lower mid strength), class VI (mild) and class VII (least potent).…”

Section: Corticosteroidsmentioning

confidence: 99%