Lecithin/chitosan nanoparticles of clobetasol-17-propionate capable of accumulation in pig skin

Şenyiğit, Taner; Sonvico, Fabio; Barbieri, Stefano; Özer, Özgen; Santi, Patrizia; Colombo, Paolo

doi:10.1016/j.jconrel.2009.11.013

Cited by 141 publications

(79 citation statements)

References 37 publications

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“…CP is the most important corticosteroid in derma- tological therapy; however, there are few reports on the quantitation of CP in skin matrices in the literature (Senyigit et al, 2010;Fontana et al, 2011;Rao, Murthy, 2005;Kalariya et al, 2005;Weigmann et al, 1999;Mueller, Anissimov, Roberts, 2003), and there are no published data on the development and validation of an analytical procedure capable of quantifying CP in both the stratum corneum and remaining skin (viable epidermis plus dermis). Literature reports on the quantitation of CP in skin are based on isocratic HPLC-RP methods, and analytical separations have been performed with water and acetonitrile as the mobile phase.…”

Section: Methods Development and Validationmentioning

confidence: 99%

“…This issue is particularly true for skin matrices, as the interactions among the analyte, skin lipids, and proteins may result in low drug recovery. High drug recovery values (above 90% from epidermis and dermis) have been reported in the literature (Senyigit et al, 2010). Weigmann et al (1999) developed an exhaustive procedure for CP extraction from human stratum corneum.…”

Section: Methods Development and Validationmentioning

confidence: 99%

“…Improvements in the safety of topical corticosteroid therapy may be achieved by drug nanoencapsulation, which can increase the drug's accumulation in the skin while minimizing deep drug permeation and adverse systemic effects (Senyigit et al, 2010). CP has been nanoencapsulated in lecithin/chitosan nanoparticles (Senyigit et al, 2010), polymer-coated lipid nanocapsules (Fontana et al, 2011), liposomes (Rao, Murthy, 2005), and lipid nanoparticles (Kalariya et al, 2005;Hu et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

“…CP has been nanoencapsulated in lecithin/chitosan nanoparticles (Senyigit et al, 2010), polymer-coated lipid nanocapsules (Fontana et al, 2011), liposomes (Rao, Murthy, 2005), and lipid nanoparticles (Kalariya et al, 2005;Hu et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

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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: Methods Development and Validationmentioning

confidence: 99%

Section: Methods Development and Validationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

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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“…15 In the literature, nanoparticles have been obtained from the supramolecular self-organizing interaction of negatively charged lipid material lecithin and the positively charged polysaccharide chitosan, without preliminary vesicle formation. [16][17][18] Diflucortolone valerate (DFV) is a potent corticosteroidal molecule which is commonly used in the treatment of skin disorders. According to the corticosteroidal classification system, DFV is classified as a high potent steroid for the available formulations of ointments and creams.…”

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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Pharmaceutical Delivery Systems Composed of Chitosan

Borgheti-Cardoso

Vicentini

Cunha-Filho

et al. 2017

Handbook of Composites From Renewable Materials

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Lecithin/chitosan nanoparticles of clobetasol-17-propionate capable of accumulation in pig skin

Cited by 141 publications

References 37 publications

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

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

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

Pharmaceutical Delivery Systems Composed of Chitosan

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