In-vitro efficacies of topical microemulsions of clotrimazole and ketoconazole; and in-vivo performance of clotrimazole microemulsion

Alam, Mohammad Mumtaz; Al-Janoobi, Fahad I.; Alzahrani, Khaled A.; Al-Agamy, Mohamed H.; Abdelgalil, Ahmed A.; Al-Mohizea, Abdullah M.

doi:10.1016/j.jddst.2017.04.025

Cited by 21 publications

(14 citation statements)

References 25 publications

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“…The reason was unclear; however, it is possible that high affinity between lipophilic CTZ and the internal oil phase of the o/w conventional cream as well as high viscosity of the cream may lead to a delay of drug release and diffusion into agar medium. It has previously been reported that some o/w ME containing CTZ could inhibit the growth of C. albicans better than conventional cream [26]. Our antifungal activity results indicate that the efficacy of CTZ against T. mentagrophytes was enhanced when ME and MBG were used as drug carriers.…”

Section: Resultssupporting

confidence: 57%

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Kaewbanjong

Amnuaikit

Souto

et al. 2018

Skin Pharmacol Physiol

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Aim: Antifungal activity, skin permeation and skin retention of water-in-oil microemulsion (ME) and microemulsion-based gel (MBG) containing clotrimazole (CTZ) were evaluated in comparison to a conventional CTZ cream. Methods: CTZ-ME and CTZ-MBG containing 1% w/w of CTZ were produced. Antifungal activity against Trichophyton mentagrophytes was assessed by the agar diffusion method. Pig skin was used in the in vitro penetration study using modified Franz diffusion cells. Drug amounts which permeated into the receptor fluid, retained in the skin membrane and remained in the donor compartment were analyzed by a validated HPLC technique. Results: CTZ-ME and CTZ-MBG exhibited inhibition zones against T. mentagrophytes whereas the conventional cream did not reveal any inhibition zone in the assay. While no CTZ was detected in the receptor fluid up to 24 h following the in vitro penetration study from all tested formulations, the amount of CTZ retained in the skin membrane when applying CTZ-ME and CTZ-MBG was remarkably higher than that when applying the cream. Conclusion: Results revealed the capacity of ME and MBG in improving skin bioavailability of CTZ while reducing the risk of systemic side effects. Thereby, ME and MBG could increase the efficacy of CTZ for dermatophytosis treatment in comparison to conventional cream.

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Section: Resultssupporting

confidence: 57%

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Kaewbanjong

Amnuaikit

Souto

et al. 2018

Skin Pharmacol Physiol

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“…This particle size and the specific coating of the droplets have a significant bearing on the longer-term stability of numerous commercial medical and non-medical products. Medical products based on nanoparticle and micrometer-scale oil droplets include therapeutic microemulsions (oil-carrying micelles), topical emulsions or creams for inflammatory skin disorders and viral infections [ 6 , 7 , 8 , 9 ]. Topical microemulsions, often referred to as swollen micelles [ 1 ], are used for the treatment of yeast infections incorporating both Tween 20 and clove oil (eugenol alcohol) formulations to give oil-based nanoparticles with a hydrodynamic diameter (diameter) of 34–50 nm [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Interfacial Effects and the Nano-Scale Disruption in Adsorbed-Layer of Acrylate Polymer-Tween 80 Fabricated Steroid-Bearing Emulsions: A Rheological Study of Supramolecular Materials

Adu-Gyamfi

Sarker

2021

Nanomaterials

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The effect of polymer adsorption on the stability and viable shelf life of 55 μm diameter oil-in-water (O/W) emulsions containing the steroid, betamethasone 21-phosphate was investigated. Two acrylate polymers, Carbopol® 971P and 974P, were added in the role of emulsion stabilizers to a model system, representing a non-ionic low molecular weight surfactant-stabilized emulsion (topically applied medicinal cream). For the purposes of this study the dosage of the viscosifier was maintained below 1% w/v and consequently, the consistency of the emulsion was measured in the diluted form. One of the polymers was responsible for elevated degrees of droplet creaming and coalescence and this was closely linked to its surface tension lowering capacity. This lowering was seen at 62 mN/m compared to the routine values at equivalent concentrations of 68 mN/m and 35 mN/m for the betamethasone drug and non-ionic surfactant-Tween 80, respectively. The same polymer also demonstrated a predisposition to form low-micron and greater sized aggregates of nanoparticles that led to extensive flocculation and the formation of a sedimentary precipitate, formed from an amalgam of the components found in the creamed droplet layer.

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“…This make it most suitable candidate in the treatment of onychomycosis [4][5][6][7][8]. For the treatment of mild-to-moderate toenail onychomycosis, Efinaconazole solution (10%, wt/wt) is already approved and available in markets of Canada, the United States, and Japan [5,9,10].…”

Section: Introductionmentioning

confidence: 99%

Development and validation of HPLC methodology for quantitative estimation of Efinaconazole in topical pharmaceutical formulation prepared in‐house for the treatment of onychomycosis

Patani

Patel

2020

Separation Science Plus

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The purpose of this research work was to design, develop, and optimize new high‐performance liquid chromatography method for quantitative estimation of Efinaconazole in topical pharmaceutical formulation developed in‐house for the treatment of onychomycosis. Based on the outcomes of preliminary investigation, optimized high‐performance liquid chromatography conditions were reverse phase column (Luna C18) as stationary material, with simple isocratic mobile phase comprising mixture of water and acetonitrile (20:80 v/v), flow rate 1 mL/min, column oven temperature 30°C, injection volume 10 µL, detection wavelength of 230 nm, and total run time of 10 min. The optimized method was successfully validated as per International Council for Harmonization guideline Q2(R1), and statistical analysis proved that the method is specific (peak purity ≥ 0.999), accurate (99.21–99.63% w/w), precise (% relative standard deviation < 2.0), and sensitive (limit of detection = 9.26 µg and limit of quantitation = 28.05 µg). As a result, this research work provides a new and simple high‐performance liquid chromatography methodology with optimized chromatographic parameters for quantitation of Efinaconazole as a routine assay purpose, contributing to the technological and scientific domain and guaranteeing a safe and effective use of Efinaconazole for the treatment of onychomycosis.

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In-vitro efficacies of topical microemulsions of clotrimazole and ketoconazole; and in-vivo performance of clotrimazole microemulsion

Cited by 21 publications

References 25 publications

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Interfacial Effects and the Nano-Scale Disruption in Adsorbed-Layer of Acrylate Polymer-Tween 80 Fabricated Steroid-Bearing Emulsions: A Rheological Study of Supramolecular Materials

Development and validation of HPLC methodology for quantitative estimation of Efinaconazole in topical pharmaceutical formulation prepared in‐house for the treatment of onychomycosis

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