Topical delivery of clobetasol propionate loaded microemulsion based gel for effective treatment of vitiligo – Part II: Rheological characterization and in vivo assessment through dermatopharmacokinetic and pilot clinical studies

Patel, Hetal; Barot, Bhavesh S.; Parejiya, Punit B.; Shelat, Pragna K.; Shukla, Arunkumar

doi:10.1016/j.colsurfb.2014.02.005

Cited by 26 publications

(14 citation statements)

References 44 publications

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“…In recent years, MEs have attracted much interest as topical drug vehicle because of their significant advantages, including thermodynamic stability, high solubilization capacities for both hydrophilic and hydrophobic molecules, easy formation, and small droplet size. In fact, ME had been widely used in pharmaceutical applications and could increase drug permeation into and through the skin (13). It is generally accepted that ME is a practical delivery platform for improving target specificity, therapeutic activity, and reducing toxicity of both hydrophilic and lipophilic substances (14)(15)(16)(17)(18)(19).…”

Section: Introductionmentioning

confidence: 99%

A Novel Topical Targeting System of Caffeine Microemulsion for Inhibiting UVB-Induced Skin Tumor: Characterization, Optimization, and Evaluation

Liu

et al. 2015

AAPS PharmSciTech

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Abstract. The purpose of the present study was to develop an optimal microemulsion (ME) formulation as topical nanocarrier of caffeine (CAF) to enhance CAF skin retention and subsequently improve its therapeutic effect on UVB-induced skin carcinogenesis. The pseudo-ternary phase diagram was developed composing of Labrafil M 1944 CS as oil phase, Cremophor EL as surfactant, tetraglycol as cosurfactant, and water. Four ME formulations at water content of 50, 60, 70, and 80% were prepared along the water dilution line of oil to surfactant ratio of 1:3 and characterized in terms of morphology, droplet size, and electric conductivity. A gel at the same drug loads (1%, w/w) was used as control. Ex vivo skin permeation studies were conducted for ME optimization. The optimized formulation (ME4) was composed of 5% (w/w) Labrafil M 1944 CS, 15% (w/w) Smix (2/1, Cremophor EL and tetraglycol), and 80% (w/w) aqueous phase. The skin location amount of CAF from ME4 was nearly 3-fold higher than control (P<0.05) with improved permeated amount through the skin. The skin targeting localization of hydrophilic substance from ME4 was further visualized through fluorescent-labeled ME by a confocal laser scanning microscope. In pharmacodynamics studies, CAF-loaded ME4 was superior in terms of increasing apoptotic sunburn cells (P<0.05) as compared with control. Overall results suggested that the ME4 might be a promising vehicle for the topical delivery of CAF.

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Section: Introductionmentioning

confidence: 99%

A Novel Topical Targeting System of Caffeine Microemulsion for Inhibiting UVB-Induced Skin Tumor: Characterization, Optimization, and Evaluation

Liu

et al. 2015

AAPS PharmSciTech

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“…The C max of PAB in the skin from ME-gel was 2.76-fold of PAB from gel (6.10 ± 2.03 µg/ml vs 2.21 ± 0.45 µg/ml), and T max from PAB ME-gel was achieved within 6 h while 7.17 h from gel, which inferred that PAB from ME-gel permeated into the skin at a faster rate than from gel (Patel., 2014). The AUC 0→12 of PAB in the skin from ME-gel was 3.02-fold of PAB from gel (41.95 ±8.89 µg/ml vs. 13.90 ± 2.22 µg/ml), which indicated the improved dermal bioavailability of PAB by ME-gel.…”

Section: Dermal Pharmacokinetics Studiesmentioning

confidence: 92%

“…However, microemulsions had very low viscosity and cannot retain at the affected position sustainably, the viscosity played an important role in promoting the drug retention in the stratum corneum and viable epidermis. Some gelling agents such as xanthan gum, carbopol, and carrageenan have been selected to increase the appropriate viscosity of ME to enhance skin permeation and retention and form microemulsion based gel (ME-gel) to improve topical applicability (Fouad et al, 2013;Gannu et al, 2010;Lapasin et al, 2001;Patel et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Microemulsion based gel for topical dermal delivery of pseudolaric acid B: In vitro and in vivo evaluation

Wan

Pan

et al. 2015

International Journal of Pharmaceutics

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“…It can be seen that the fluorescein spread everywhere, without binding to any cellular structure or appendices. This demonstrates that such colloidal drug delivery system can target the absorption and penetration of a drug in specific skin layers, i.e the SC and the epidermis, as desired [42].…”

Section: Confocal Laser Scanning Microscopy (Clsm)mentioning

confidence: 94%

Prolonged skin retention of clobetasol propionate by bio-based microemulsions: a potential tool for scalp psoriasis treatment

Langasco

Tanrıverdi

Özer

et al. 2017

Drug Development and Industrial Pharmacy

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Novel effective and cosmetically acceptable formulations are needed for the treatment of scalp psoriasis, due to the poor efficacy of the current products. The challenge in developing safe, efficient, and convenient delivery systems for this drug was addressed in the present work by formulating clobetasol propionate-loaded W/O microemulsions (MEs). Pseudo-ternary phase diagrams were constructed by using a combination of biocompatible and biodegradable excipients. Characterization studies demonstrated that selected MEs had suitable technological features such as being Newtonian fluids, possessing low viscosity, and high thermodynamic stability. Photomicrographs showed a significant alteration of the skin structure after treatment with MEs, and a preferential concentration of these in the stratum corneum and epidermis. These data, together with ex vivo permeation results, suggested an enhanced topical targeted effect due to an increased drug retention efficacy in the upper skin layers, as desired. Moreover, the bio-based excipients selected could contribute to the healing of the psoriatic scalp. In this way, the improvement of clobetasol efficacy is combined with the useful properties of the microemulsion components and with environmental safety.

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Topical delivery of clobetasol propionate loaded microemulsion based gel for effective treatment of vitiligo – Part II: Rheological characterization and in vivo assessment through dermatopharmacokinetic and pilot clinical studies

Cited by 26 publications

References 44 publications

A Novel Topical Targeting System of Caffeine Microemulsion for Inhibiting UVB-Induced Skin Tumor: Characterization, Optimization, and Evaluation

A Novel Topical Targeting System of Caffeine Microemulsion for Inhibiting UVB-Induced Skin Tumor: Characterization, Optimization, and Evaluation

Microemulsion based gel for topical dermal delivery of pseudolaric acid B: In vitro and in vivo evaluation

Prolonged skin retention of clobetasol propionate by bio-based microemulsions: a potential tool for scalp psoriasis treatment

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