In vitro evaluation of transdermal nicotine delivery systems commercially available in Brazil

Ruela, André Luís Morais; Figueiredo, Eduardo Costa; Perissinato, Aline Gravinez; Lima, Ana Carolina Zogbi; Araújo, Magali Benjamim; Pereira, Gislaine Ribeiro

doi:10.1590/s1984-82502013000300020

Cited by 16 publications

(15 citation statements)

References 17 publications

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Section: In Vitro Evaluation Of the Skin Permeation Of Drugsmentioning

confidence: 99%

“…These evaluations may be performed in vitro after the skin permeation assays using diffusion cells (Reid et al, 2013, Ruela et al, 2013Paleco et al, 2014;Shah et al, 2015). Animal models (mice or rats) have been employed for in vivo evaluations.…”

Section: Studies Of Cutaneous Retentionmentioning

confidence: 99%

“…Selective analytical techniques are used for appropriate separation of contaminants from the skin, formulation, or receptor medium. High-performance liquid chromatography (HPLC) is recommended for drug quantification (Siewert et al, 2003;Thakker, Chern, 2003;Wang, Ma, Higgins, 2006;Hanson, 2010;Ruela et al, 2013;Selzer et al, 2013).The Keshary-Chien cell is an experimental apparatus for evaluation of poorly water-soluble drugs, which assures sink conditions. The apparatus has the same configuration as that of the vertical diffusion cell; however, it can increase the homogeneity of larger volumes (>15 mL) of the receptor medium (Tojo, Keshary, Chien, 1986).…”

mentioning

confidence: 99%

“…Drug quantification is performed by using selective and validated analytical methods. In general, HPLC is the analytical technique usually employed (Ruela et al, 2013).Presently, there is a trend in replacement methods for animal experimentation, and 3D in vitro reconstructed human skin models are alternatives to animal testing (Gotz et al, 2012;Dos Santos et al, 2015). Three-dimensional (3D) in vitro skin models have been employed in both academic and research laboratories of skin-related industries to evaluate the toxicity and efficacy of drugs, drug products, and cosmetics and to study interactions between skin and its microbiome (Bojar, 2015;Dos Santos et al, 2015).…”

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confidence: 99%

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Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

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197

114

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The skin barrier function has been attributed to the stratum corneum and represents a major challenge in clinical practice pertaining to cutaneous administration of drugs. Despite this, a large number of bioactive compounds have been successfully administered via cutaneous administration because of advances in the design of topical and transdermal formulations. In vitro and in vivo evaluations of these novel drug delivery systems are necessary to characterize their quality and efficacy. This review covers the most well-known methods for assessing the cutaneous absorption of drugs as an auxiliary tool for pharmaceutical formulation scientists in the design of drug delivery systems. In vitro methods as skin permeation assays using Franz-type diffusion cells, cutaneous retention and tape-stripping methods to study the cutaneous penetration of drugs, and in vivo evaluations as pre-clinical pharmacokinetic studies in animal models are discussed. Alternative approaches to cutaneous microdialysis are also covered. Recent advances in research on skin absorption of drugs and the effect of skin absorption enhancers, as investigated using confocal laser scanning microscopy, Raman confocal microscopy, and attenuated total reflectance Fourier-transform infrared spectroscopy, are reviewed. Uniterms:Skin absorption/effects/study. Skin absorption/topical formulations. Skin absorption/ transdermal formulations. Skin absorptions/enhancers. INTRODUCTIONTopical and transdermal drug delivery systems have shown significant advantages in clinical practice for drug targeting to the action site in the body; this has reduced the systemic side effects. The administration of drugs by through the skin is also performed to achieve controlled or prolonged drug delivery, and this route can be explored as an alternative to the oral route. The oral route shows some limitations for drugs with irregular absorption in the gastrointestinal tract and low bioavailability and for drugs with increased first pass metabolism and short plasma halflife times (Barry, 2001;Wokovich et al., 2006;Prausnitz, Langer, 2009;Alexander et al., 2012).Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected. This is the case for topical formulations for treatment of skin disorders such as acne and cutaneous inflammatory diseases that include dermatitis, erythematous lupus, and psoriasis. On the other hand, transdermal formulations release drugs that permeate through the skin and enter the systemic circulation. Transdermal therapy must ensure that significant concentrations of the drug are absorbed to reach effective plasma concentrations. Permeation of drugs is targeted in some cases to body regions close to the action site, where a regional effect is expected, e.g., in the muscles, blood vessels, and articulations. In this way, the term "cutaneous absorption" is properly used to characterize the sum of the amounts of drug that penetrate and permeate the skin (Barry, 2001;El Maghraby, Barry;Willi...

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Section: In Vitro Evaluation Of the Skin Permeation Of Drugsmentioning

confidence: 99%

Section: Studies Of Cutaneous Retentionmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

Self Cite

197

114

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“…Correspondingly, transdermal nicotine patches available in the Brazilian market, including a rate-controlling membrane device (15 cm 2 of patch size containing 78 mg of drug) and a polymeric matrix device (20 cm 2 of patch size containing 35 mg of drug) showed permeation rates of 41.7 ± 1.2 µg.cm -2 .h -1 and 38.3 ± 3.6 µg.cm -2 .h -1 , respectively (Ruela et al, 2013). Vitamin E TGPS cubic phase system developed promoted a lower cumulative amount of permeated nicotine per cm² and lower release rate (138.86 ± 20.44 μg.cm -2 after 12 h and 10.48 µg.cm -2 .h -1 ) compared with marketed patches, but comparable released percentage amounts (65.54% of the initial content).…”

Section: Discussionmentioning

confidence: 99%

Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

Borgheti-Cardoso

Vicentini

Gratieri

et al. 2016

Braz. J. Pharm. Sci.

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Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p < 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm 2 , respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm 2 , respectively). Further studies to evaluate skin sensitization and irritation are now necessary.Uniterms: Nicotine/transdermal patches. Nicotine/controlled transdermal delivery. Liquid crystalline systems/development. Vitamin E TPGS. Skin irritation/control/in vitro study. Skin irritation/use of transdermal patches.Adesivos transdérmicos de nicotina são utilizados para cessação de fumar, tratamento de problemas de pele com infiltração de eosinófilos e para melhorar a atenção em pacientes com doença de Alzheimer e enfraquecimento da memória associada à idade. No entanto, a irritação da pele com o uso prolongado dos adesivos ainda é um problema. O objetivo deste trabalho foi desenvolver sistema líquido cristalino (SLC) de preparo simples contendo vitamina E TPGS capaz de controlar a liberação de nicotina e reduzir os problemas de irritação cutânea. Os SLCs foram caracterizados por análise visual e microscopia de luz polarizada. As administrações tópica e transdérmica de nicotina foram investigadas in vitro utilizando pele de orelha de porco em célula de difusão de Franz. A permeação da nicotina veiculada pela fase cúbica desenvolvida seguiu cinética de ordem zero (r = 0,993) e foi significativamente maior do que o controle (solução de nicotina) após 12 h (p < 0,05) (138,86 ± 20,44 e 64,91 ± 4,06 µg/cm 2 , respectivamente). A fase cúbica também promoveu aumento da penetração de nicotina nas camadas viáveis da pele quando comparado ao controle (8,18 ± 1,89 e 2,63 ± 2,51 µg/cm 2 , respectivamente). Estudos futuros para avaliar a sensibilização e irritação da pele são necessários.

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Design and Evaluation of Molecularly Imprinted Polymers as Drug Delivery Systems

Ruela

Pereira

2016

Advanced Molecularly Imprinting Materials

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In vitro evaluation of transdermal nicotine delivery systems commercially available in Brazil

Cited by 16 publications

References 17 publications

Evaluation of skin absorption of drugs from topical and transdermal formulations

Evaluation of skin absorption of drugs from topical and transdermal formulations

Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

Design and Evaluation of Molecularly Imprinted Polymers as Drug Delivery Systems

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