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      In vivo determination of the diclofenac skin reservoir: comparison between passive, occlusive, and iontophoretic application

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          Abstract

          Aim

          There is scarce information concerning the pharmacodynamic behavior of topical substances used in the physiotherapy setting. The aim of the present study was to estimate the formation and emptying of the diclofenac (DF) skin reservoir after passive, semiocclusive, and electrically assisted applications of DF.

          Subjects and methods

          Five different groups of healthy volunteers (n total=60, 23 male and 37 female), participated in this study. A 1% DF (Voltaren Emulgel) formulation (12 mg) was applied on the volar forearms on randomized defined circular skin areas of 7 cm 2. DF was applied for 20 minutes under three different conditions at the same time. The presence of DF in the skin results in a reduction of the methyl nicotinate (MN) response. To estimate the bioavailability of DF in the skin, MN responses at different times following initial DF application (1.5, 6, 24, 32, 48, 72, 96, and 120 hours) were analyzed.

          Results

          At 1.5 hours after the initial DF application, a significant decrease in MN response was detected for the occluded and iontophoretic delivery. Passive application resulted in a decrease of the MN response from 6 hours post-DF application. The inhibition remained up to 32 hours post-DF application for the iontophoretic delivery, 48 hours for the occluded application, and 72 hours for the passive delivery. At 96 and 120 hours post-DF application none of the MN responses was inhibited.

          Conclusion

          The formation and emptying of a DF skin reservoir was found to be dependent on the DF-application mode. Penetration-enhanced delivery resulted in a faster emptying of the reservoir.

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          Most cited references 29

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          Skin color measurements: comparison between three instruments: the Chromameter(R), the DermaSpectrometer(R) and the Mexameter(R).

          BACKGROUND/AIMS: Two types of skin reflectance instruments are available nowadays for the determination of skin color: a tristumulus colorimeter (Chromameter from Minolta) using the CIE L*a*b* color system and the narrow-band simple reflectance meters (DermaSpectrometer from Cortex and Mexameter from Courage-Khazaka) using the erythema/melanin indices. The purpose of this study was to compare the capabilities of the three instruments (sensitivity, repeatability and correlation) in vitro and in vivo. METHODS: Comparative color measurements were carried out first in vitro on standardized color charts and subsequently in vivo on different skin areas in human volunteers. Skin color changes induced by various physico-chemical treatments were also quantitatively evaluated with the three instruments. RESULTS: The in vitro and in vivo repeatabilty as well as the sensitivity of the three instruments are rather good. Erythema and skin blanching could be readily quantified by the increase of the a* parameter and of the erythema indices of the simple reflectance meters. Natural UV tanning and artificial chemical tanning could be measured by the decrease of L* and increase of b* and of the melanin indices. CONCLUSION: The Chromameter and the two narrow-band reflectance instruments were able to characterize skin color and to quantify small skin color changes. Moderate to high significant linear correlations could be established between the CIE L*a*b* color parameters and the erythema/melanin indices.
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            Liposomal systems as drug delivery vehicles for dermal and transdermal applications.

            Enhancement strategies are necessary to improve the dermal/transdermal bioavailability of drugs applied to the skin due to its amazing barrier, the stratum corneum. Strategies to overcome this barrier, thus improving drug release to the skin include the use of penetration enhancers, specific delivery systems, supersaturated solutions and physical methods (iontophoresis, electroporation and ultrasound). Delivery of active agents to the skin by liposomal carriers has improved topical therapy in the field of dermatology. The interest in these carriers is based on their potential to enclose various types of biological materials and to deliver them to diverse cell types. Particularly, in recent years liposomes have been shown to be a promising drug-delivery system to the skin. Their use may produce several-fold higher drug concentrations in the epidermis and dermis and lower systemic concentrations when compared to conventional dosage forms. On the other hand, special characteristic vesicles like ethosomes, transfersomes and niosomes may be potential transdermal delivery systems for ionic molecules and polypeptides.
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              • Article: not found

              Skin color measurements in terms of CIELAB color space values.

              The principles of color measurement established by the Commission International d'Eclairage have been applied to skin and the results expressed in terms of color space L*, hue angle, and chroma values. The distribution of these values for the ventral forearm skin of a sample of healthy volunteers is presented. The skin-color characteristics of a European subgroup is summarized and briefly compared with others. Color differences between individuals were identified in terms of one, two, or all three color-space parameters. Because the method is quantitative and the principles internationally recognized, these color-space parameters are proposed for the unambiguous communication of skin-color information that relates directly to visual observations of clinical importance or scientific interest.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2015
                13 February 2015
                : 9
                : 835-840
                Affiliations
                [1 ]Department of Health Sciences, University of Applied Sciences and Arts of Southern Switzerland, Landquart, Switzerland
                [2 ]Faculty of Physical Education and Physiotherapy, Vrije Universiteit Brussel, Brussels, Belgium
                Author notes
                Correspondence: Ron Clijsen, Department of Health Sciences, University of Applied Sciences and Arts of Southern Switzerland, Weststrasse 8, CH-7302 Landquart, Switzerland, Tel +41 81 300 0175, Fax +41 81 300 0171, Email contact ron.clijsen@ 123456vub.ac.be
                Article
                dddt-9-835
                10.2147/DDDT.S76002
                4335612
                © 2015 Clijsen et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

                The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

                Categories
                Original Research

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