Effect of permeation enhancers on the iontophoretic transport of metoprolol tartrate and the drug retention in skin

Nair, Anroop B.; Vyas, Hiral; Shah, Jigar; Kumar, Ashok

doi:10.3109/10717544.2010.509361

Cited by 42 publications

(24 citation statements)

References 26 publications

(27 reference statements)

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“…In general, drug reservoir in the skin layers is likely to release over an extended period of time (Zhai, Maibach, 2004;Nair et al, 2011;Nair et al, 2012). Recently, the application of iontophoresis to create depot of acyclovir was reported which would be beneficial for the effective treatment of viral infections by providing sustained release of drug over an extended period (Anderson et al, 2003).…”

Section: Drug Depot In Skinmentioning

confidence: 99%

Basic considerations in the dermatokinetics of topical formulations

Nair

Jacob

Al‐Dhubiab

et al. 2013

Braz. J. Pharm. Sci.

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Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form. However, determining drug concentration in the skin layers following topical application of dermatological formulations is a great challenge. The protocols followed in oral formulations could not be applied for topical dosage forms. The regulatory agencies are considering several possible approaches such as tape stripping, microdialysis etc. On the other hand, the skin bioavailability assessment of xenobiotics is equally important for topical formulations in order to evaluate the toxicity. It is always possible that drug molecules applied on the skin surface may transport thorough the skin and reaches systemic circulation. Thus the real time measurement of molecules in the skin layer has become obligatory. In the last two decades, quite a few investigations have been carried out to assess the skin bioavailability and toxicity of topical/dermatological products. This review provides current understanding on the basics of dermatokinetics, drug depot formation, skin metabolism and clearance of drug molecules from the skin layers following application of topical formulations.Uniterms: Dermatological formulations/pharmacokinetics. Dermatological formulations/ toxicity. Dermatokinetics. Skin/metabolism. Microdialysis. Tape stripping.A avaliação da biodisponibilidade de moléculas de fármacos no sítio de ação oferece melhor compreensão sobre a eficiência da forma de dosagem. Entretanto, a determinação da concentração de fármaco nas camadas da pele em seguida à aplicação tópica de formulações dermatológicas é um grande desafio. Os protocolos seguidos para as formulações orais não podem ser aplicados para as formulações tópicas. As agências regulatórias consideram várias abordagens possíveis, tape stripping, microdiálise etc. Por outro lado, a avaliação da biodisponibilidade de xenobióticos na pele é igualmente importante para as formulações tópicas para se avaliar a toxicidade. É sempre possível que as moléculas de fármaco aplicadas na superfície da pele sejam transportadas através da pele e alcancem a circulação sistêmica. Assim, a medida em tempo real de moléculas na camada da pele tem se tornado obrigatória. Nas últimas duas décadas, realizaram-se poucas pesquisas para avaliar a biodisponibilidade da pele e a toxicidade de produtos tópicos/dermatológicos. Esta revisão fornece a compreensão atual com base na dermatocinética, formação de fármaco de depósito, metabolismo da pele e o clearance das moléculas de fármaco das camadas da pele em seguida à aplicação de formulações tópicas.Unitermos: Formulações dermatológicas/farmacocinética. Formulações dermatológicas/toxicidade. Dermatocinética Pele/metabolismo. Microdiálise. Tape stripping.

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Section: Drug Depot In Skinmentioning

confidence: 99%

Basic considerations in the dermatokinetics of topical formulations

Nair

Jacob

Al‐Dhubiab

et al. 2013

Braz. J. Pharm. Sci.

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“…Therefore, various techniques are used to enhance transdermal drug permeation, including the use of nanocarriers (e.g. microemulsions, nanoparticles and liposomes), penetration enhancers and physical techniques, such as iontophoresis, microneedles and electroporation, alone or in combination with other method (Essa et al, 2004;Wang et al, 2007;Balaguer-Fernandez et al, 2010;Vaghani et al, 2010;Nair et al, 2011). Drug carriers, such as microemulsions, nanoparticles and liposomes are a common and useful for transdermal drug delivery as they can alter the physical characteristics of applied drug and increases its transport across the skin (Nicoli et al, 2001;Lee & Langer, 2003;Essa et al, 2004;Liu et al, 2008;Xing et al, 2009;Tsai et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

et al. 2017

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Agomelatine is a new antidepressant having very low oral drug bioavailability less than 5% due to being liable to extensive hepatic 1st pass effect. This study aimed to deliver agomelatine by transdermal route through formulation and optimization of microemulsion gel. Pyramidal screening was performed to select the most suitable ingredients combinations and then, the design expert software was utilized to optimize the microemulsion formulations. The independent variables of the employed mixture design were the percentages of capryol 90 as an oily phase (X 1 ), Cremophor RH40 and Transcutol HP in a ratio of (1:2) as surfactant/cosurfactant mixture 'S mix ' (X 2 ) and water (X 3 ). The dependent variables were globule size, optical clarity, cumulative amount permeated after 1 and 24 h, respectively (Q1 and Q 24 ) and enhancement ratio (ER). The optimized formula was composed of 5% oil, 45% S mix and 50% water. The optimized microemulsion formula was converted into carbopol-based gel to improve its retention on the skin. It enhanced the drug permeation through rat skin with an enhancement ratio of 37.30 when compared to the drug hydrogel. The optimum ME gel formula was found to have significantly higher C max , AUC 0-24 h and AUC 0-1 than that of the reference agomelatine hydrogel and oral solution. This could reveal the prosperity of the optimized microemulsion gel formula to augment the transdermal bioavailability of agomelatine. ARTICLE HISTORY

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“…In the past decade, numerous strategies have been investigated for their ability to increase drug permeation capacity through the skin, including vehicles, chemical penetration enhancers, iontophoresis, electroporation, ultrasound, and microneedle technologies, used alone or in combination. [11][12][13][14][15] In recent years, ethosomes, microemulsions, liposomes, and polymeric nanoparticles have shown potential as drug vehicles in modifying the properties of therapeutic agents and in improving their transport through the skin. [16][17][18][19][20][21] M i c r o e m u l s i o n s a r e o p t i c a l ly i s o t r o p i c a n d thermodynamically stable colloidal systems.…”

Section: Introductionmentioning

confidence: 99%

Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

Huang¹,

Tsai²,

Lin³

et al. 2013

IJN

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Abstract:The aim of this study was to evaluate the potential of microemulsions as a drug vehicle for transdermal delivery of citalopram. A computerized statistical technique of response surface methodology with mixture design was used to investigate and optimize the influence of the formulation compositions including a mixture of Brij 30/Brij 35 surfactants (at a ratio of 4:1, 20%-30%), isopropyl alcohol (20%-30%), and distilled water (40%-50%) on the properties of the drug-loaded microemulsions, including permeation rate (flux) and lag time. When microemulsions were used as a vehicle, the drug permeation rate increased significantly and the lag time shortened significantly when compared with the aqueous control of 40% isopropyl alcohol solution containing 3% citalopram, demonstrating that microemulsions are a promising vehicle for transdermal application. With regard to the pharmacokinetic parameters of citalopram, the flux required for the transdermal delivery system was about 1280 µg per hour. The microemulsions loaded with citalopram 3% and 10% showed respective flux rates of 179.6 µg/cm 2 and 513.8 µg/cm 2 per hour, indicating that the study formulation could provide effective therapeutic concentrations over a practical application area. The animal study showed that the optimized formulation (F15) containing 3% citalopram with an application area of 3.46 cm 2 is able to reach a minimum effective therapeutic concentration with no erythematous reaction.

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Effect of permeation enhancers on the iontophoretic transport of metoprolol tartrate and the drug retention in skin

Cited by 42 publications

References 26 publications

Basic considerations in the dermatokinetics of topical formulations

Basic considerations in the dermatokinetics of topical formulations

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

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