Combined chemical and electrical enhancement modulates stratum corneum structure

Graaff, Anko M. de; Li, G.L.; Aelst, A.C. van; Bouwstra, Joke A.

doi:10.1016/s0168-3659(03)00134-2

Cited by 16 publications

(7 citation statements)

References 20 publications

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“…Cumulative corrections were made to obtain the total amount of drug diffused at each time interval and ex vivo parameters were calculated. The average cumulative amount of drug permeated per unit surface area of the skin was plotted versus time [6]. The slope of the linear portion of the plot was calculated as flux J ss ( μ g/cm 2 /h), and the permeability coefficient was calculated using the following formula:

\begin{matrix} K_{p} = \frac{J_{ss}}{c_{v}}, \end{matrix}

where K p is the permeability coefficient and C v is the total amount of drug.…”

Section: Methodsmentioning

confidence: 99%

Optimization of Metronidazole Emulgel

Rao¹,

Sukre²,

Aghav³

et al. 2013

Journal of Pharmaceutics

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The purpose of the present study was to develop and optimize the emulgel system for MTZ (Metronidazole), a poorly water soluble drug. The pseudoternary phase diagrams were developed for various microemulsion formulations composed of Capmul 908 P, Acconon MC8-2, and propylene glycol. The emulgel was optimized using a three-factor, two-level factorial design, the independent variables selected were Capmul 908 P, and surfactant mixture (Acconon MC8-2 and gelling agent), and the dependent variables (responses) were a cumulative amount of drug permeated across the dialysis membrane in 24 h (Y 1) and spreadability (Y 2). Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equations were generated for responses Y 1 and Y 2. The statistical validity of the polynomials was established, and optimized formulation factors were selected. Validation of the optimization study with 3 confirmatory runs indicated a high degree of prognostic ability of response surface methodology. Emulgel system of MTZ was developed and optimized using 23 factorial design and could provide an effective treatment against topical infections.

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\begin{matrix} K_{p} = \frac{J_{ss}}{c_{v}}, \end{matrix}

where K p is the permeability coefficient and C v is the total amount of drug.…”

Section: Methodsmentioning

confidence: 99%

Optimization of Metronidazole Emulgel

Rao¹,

Sukre²,

Aghav³

et al. 2013

Journal of Pharmaceutics

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“…The average cumulative amount of the drug permitted through the unit surface of the skin was plotted against time in an hour. From the plot, the slope of the linear portion was calculated [22]. It was considered as flux Jss (µg/cm 2 /hr).…”

Section: Ex-vivo Diffusion Studiesmentioning

confidence: 99%

“…Qs to 100 28.00 0.043 b 13 78.00 −9.750E-003 b 23 −7.75 0.062 b 11 18.13 −0.065 b 22 −46.12 0.11 b 33 5.37 0.065 It is expressed to understand the maximum surface area of the skin, in which the formulation spreads over. On the contrary, spread ability has a direct impact on drug distribution and penetration throughout the skin.…”

Section: Spread Ability Studiesmentioning

confidence: 99%

Formulation and Optimization of Celecoxib Nanoemulgel

Bhattacharya

Prajapati

2017

Asian J Pharm Clin Res

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Objective: The main objective of this experiment was to prepare and optimized celecoxib nanoemulgel. This formulation can be used for acute rheumatoid arthritis patients. Methods:Celecoxib is a poorly water soluble drug. We prepared celecoxib nanoemulgel to improve intrinsic solubility of celecoxib and enhance deeper permeation throughout the skin. After several screening, the combination of acetonitrile, triacetin, campul 908P was considered for oil phase; acconon MC8-2EP as surfactant, and capmul MCM C-10 as a co-surfactant accordingly. As per Box-Behnken surface design model, optimization was done for all the 13 formulations.Results: Based on pseudo ternary plot, it was found that 4:1 S mix ratio was optimum and possessed maximum drug solubility. Further, screening shown, 0.25-0.75% carbopol-940 can be a stable candidate for hydrogel preparation. Prepared nanoemulsions and hydrogels were admixed to prepare nanoemulgel. Based on overlay plot, EG14* formulation was consider as optimum one, and various evaluation parameters were performed along with other formulations. Using Franz diffusion cell, in-vitro diffusion studies was performed. Almost all the formulations produces good qualitative drug release profile. The EG14* shown 95.50% drug release after 12 th hrs with standard Higuchi plot (R 2 value 0.9989). The optimum viscosity was found to be 521±0.81 mPas at 100 rpm. The appearance of the formulations was milky, yellowish white with expectable pH ranged from 5.8 to 6.7. The optimized formulation has good spreadability coefficient, good ex-vivo diffusion enhancement factor (3.03) as compare to marketed gel. Mostly, our formulations have less skin irritation and higher anti-inflammatory activity (92.56% of inhibition of paw edema for EG14*). Conclusion:From the thermodynamic studies, it was confirmed that EG14* maintained excellent stability profile in various heating-cooling cycle, centrifugation, and freeze-thaw cycle condition. Hence, it can be conclude that, our formulation, can be consider for pilot scale up.

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“…Iontophoresis has potential to overcome many barriers associated with transdermal delivery of drugs and it also broadens the spectrum of drugs that can be delivered via skin, increases systemic treatment efficacy therefore, this method of transport is in high demand for increasing permeation. [1][2][3] Iontophoresis uses a small electrical current to enhance the transport of both ionic and nonionic molecules across the skin in controlled and programmable manner. 4,5 The enhancement of drug due to this method results from a number of possible mechanisms including the ion-electric field interaction (electrorepulsion), 5 convective flow (electro-osmosis) 6 and current-induced 7 increase in skin permeability.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Passive and Iontophoretic Transport of Lisinopril from Hydrogel Matrix Across Model Membrane In Vitro

Faruk¹,

Ishar²

2010

IJDDT

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Clinical studies of lisinopril delivery through iontophoresis are highly desired for better controls over transdermal drug flux. Therefore, investigations were carried out to ascertain the relative importance of the various factor for iontophoretic transport using an ionizable drug lisinopril, which has four pKa values 2.4, 4.0 (for amino group) and 6.7, 7.0 (for carboxylic group). Ionization of lisinopril varies with pH, hence rate and extent of transport across the skin can be enhanced, controlled and manipulated by the application of factors like anodal and cathodal current at varied pH of donor solution and current densities. To determine these parameters, experiments were performed and data were collected at 3.0, 4.0 and 7.4 pH using 4 mg/ml drug concentration and 0.1 mA/cm2 current density for 10 hours. After establishing the pH for optimum transport of drug, effect of current density (0.1, 0.2, 0.3 and 0.4 mA/cm2) on the transport of drug (keeping drug concentration constant) were investigated. Passive diffusion of lisinopril was maximal at pH 3.0, when unionized form of drug was 45%. Anodal iontophoresis was most effective (significant result, p less than 0.05) in transport of drug across skin as compared to cathodal iontophoresis at pH 3.0. While at pH 4.0, cathodal iontophoretic transport of lisinopril across rat skin was highly effective (Student‘t’ test, p less than 0.05) compared to anodal iontophoresis. The effect of current density on steady state flux of lisinopril during cathodal iontophoresis at 7.4 pH was 1.33 ± 1.12 and 24.8 ± 3.1 μg/cm2/h at 0.0 under passive diffusion and 4 mA/cm2, respectively. Thus, flux was enhanced nearly 18.6 times during anodal iontophoresis as compared to passive diffusion. For cathodal flux at pH 3.0 on similar iontophoretic treatment showed enhancement nearly 4 times.

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Combined chemical and electrical enhancement modulates stratum corneum structure

Cited by 16 publications

References 20 publications

Optimization of Metronidazole Emulgel

Optimization of Metronidazole Emulgel

Formulation and Optimization of Celecoxib Nanoemulgel

Evaluation of Passive and Iontophoretic Transport of Lisinopril from Hydrogel Matrix Across Model Membrane In Vitro

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