Combined strategies for enhancing the transdermal absorption of midazolam through human skin

Balaguer-Fernández, C.; Femenía-Font, A.; Muedra, Vicente; Merino, Virginia; López-Castellano, Alicia

doi:10.1111/j.2042-7158.2010.01142.x

Cited by 13 publications

(11 citation statements)

References 36 publications

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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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Section: Introductionmentioning

confidence: 99%

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

et al. 2017

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“…This technique enables the transdermal delivery of hydrophilic charged molecules compared with the conventional passive transdermal approach. 19,20) In the present study, the permeation of glycyrrhizin through porcine skin was observed in the range of applied current intensity, from 0.125 to 0.5 mA/ cm 2 . When no current was applied, the amount of glycyrrhizin permeated was less than the LOQ of the analysis.…”

Section: Discussionmentioning

confidence: 99%

Iontophoretic Transdermal Delivery of Glycyrrhizin: Effects of pH, Drug Concentration, Co-ions, Current Intensity, and Chemical Enhancers

Yamamoto¹,

Takasuga²,

Kominami³

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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The aim of the present study was to evaluate the feasibility of transdermal delivery of glycyrrhizin, an agent used in the treatment of chronic hepatitis C, by cathodal iontophoresis using Ag/AgCl electrodes in vitro. The effects of donor pH (pH 4-7), concentration of drug (0.025-0.2% (w/v)), concentration of external chloride ions (Cl ) (0-133 mM), current strength (0-0.5 mA/cm 2 ), and permeation enhancers (urea and Tween 80) on the skin permeability of glycyrrhizin were examined in in vitro skin permeation studies using porcine ear skin as the membrane. The cumulative amount of permeated glycyrrhizin and the steady-state skin permeation flux of glycyrrhizin across porcine skin increased in a pH-dependent manner. The skin permeability of glycyrrhizin was independent of the concentration of drug and competed only with a high external Cl concentration. The skin permeation flux of glycyrrhizin increased with the current (R 2 0.8955). The combination of iontophoresis and enhancers provided an additive or synergistic effect, and a skin permeation flux of about 60 µg/h/cm 2 was achieved. The plasma concentration of glycyrrhizin in humans, extrapolated from the in vitro steady-state permeation flux across porcine skin, was within the therapeutic level. These results suggest that cathodal iontophoresis can be used as a transdermal drug delivery system for glycyrrhizin using reasonable patch sizes and acceptable levels of current intensity.

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“…It is difficult to exploit the transdermal route to deliver therapeutic amounts of tramadol by conventional passive transdermal administration, since tramadol hydrochloride is hydrophilic (log P at pH 7.0 is 1.35) and its oral daily dose is quite large (50–400 mg) with high bioavailability (∼70%) [3,4] . Iontophoresis is a technique used to enhance the transdermal delivery of compounds through the skin via application of a small electric current, and enables transdermal delivery of relatively large amounts of hydrophilic charged molecules compared with the conventional passive transdermal approach [16–18,33] . The pKa of tramadol hydrochloride is 9.41, and so anodal iontophoresis of tramadol hydrochloride is probably the most promising transdermal drug delivery system to attain therapeutic blood levels of tramadol.…”

Section: Discussionmentioning

confidence: 99%

“…[3,4] Iontophoresis is a technique used to enhance the transdermal delivery of compounds through the skin via application of a small electric current, and enables transdermal delivery of relatively large amounts of hydro-philic charged molecules compared with the conventional passive transdermal approach. [16][17][18]33] The pKa of tramadol hydrochloride is 9.41, and so anodal iontophoresis of tramadol hydrochloride is probably the most promising transdermal drug delivery system to attain therapeutic blood levels of tramadol.…”

Section: Discussionmentioning

confidence: 99%

In-vitro and in-vivo transdermal iontophoretic delivery of tramadol, a centrally acting analgesic

Takasuga¹,

Yamamoto²,

Mafune³

et al. 2011

Journal of Pharmacy and Pharmacology

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Combined strategies for enhancing the transdermal absorption of midazolam through human skin

Cited by 13 publications

References 36 publications

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

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

Iontophoretic Transdermal Delivery of Glycyrrhizin: Effects of pH, Drug Concentration, Co-ions, Current Intensity, and Chemical Enhancers

In-vitro and in-vivo transdermal iontophoretic delivery of tramadol, a centrally acting analgesic

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