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      Lecithin-Linker Microemulsion Gelatin Gels for Extended Drug Delivery

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          Abstract

          This article introduces the formulation of alcohol-free, lecithin microemulsion-based gels (MBGs) prepared with gelatin as gelling agent. The influence of oil, water, lecithin and hydrophilic and lipophilic additives (linkers) on the rheological properties and appearance of these gels was systematically explored using ternary phase diagrams. Clear MBGs were obtained in regions of single phase microemulsions (μEs) at room temperature. Increasing the water content in the formulation increased the elastic modulus of the gels, while increasing the oil content had the opposite effect. The hydrophilic additive (PEG-6-caprylic/capric glycerides) was shown to reduce the elastic modulus of gelatin gels, particularly at high temperatures. In contrast to anionic (AOT) μEs, the results suggest that in lecithin (nonionic) μEs, the introduction of gelatin “dehydrates” the μE. Finally, when the transdermal transport of lidocaine formulated in the parent μE and the resulting MBG were compared, only a minor retardation in the loading and release of lidocaine was observed.

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          Most cited references79

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          Solute Diffusion within Hydrogels. Mechanisms and Models

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            Porcine ear skin: an in vitro model for human skin.

            Porcine ear skin is used in studies of percutaneous penetration as a substitute for human skin. The structure of this tissue, including hair follicles, was studied qualitatively and quantitatively in comparison with human skin. Sections of shock-frozen biopsies, biopsies embedded in paraffin and cyanoacrylate skin surface biopsies were investigated using microscopy. The thickness of the different skin layers and the follicular characteristics were determined. The thickness of the stratum corneum was 17-28 microm, whereas the viable epidermis was 60-85 microm thick. On 1 cm(2), 11-25 hairs were detected, showing a diameter of 58-97 microm and a maximal extension depth of 0.96-1.38 mm into the skin. The orifices of the porcine infundibula showed a diameter of approximately 200 microm. The results obtained are similar to those of human skin, indicating the suitability of this porcine tissue as a model for human skin.
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              Influence of microemulsions on cutaneous drug delivery.

              In attempt to increase cutaneous drug delivery, microemulsion vehicles have been more and more frequently employed over recent years. Microemulsion formulations have been shown to be superior for both transdermal and dermal delivery of particularly lipophilic compounds, but also hydrophilic compounds appear to benefit from application in microemulsions compared to conventional vehicles, like hydrogels, emulsions and liposomes. The favourable drug delivery properties of microemulsions appear to mainly be attributed to the excellent solubility properties. However, the vehicles may also act as penetration enhancers depending on the oil/surfactant constituents, which involves a risk of inducing local irritancy. The correlation between microemulsion structure/composition and drug delivery potential is not yet fully elucidated. However, a few studies have indicated that the internal structure of microemulsions should allow free diffusion of the drug to optimise cutaneous delivery from these vehicles.
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                Author and article information

                Journal
                Pharmaceutics
                Pharmaceutics
                pharmaceutics
                Pharmaceutics
                MDPI
                1999-4923
                31 January 2012
                March 2012
                : 4
                : 1
                : 104-129
                Affiliations
                Department of Chemical Engineering and Applied Chemistry, University of Toronto, Toronto, ON M5S 3E5, Canada
                Author notes
                [* ] Author to whom correspondence should be addressed; Email: edgar.acosta@ 123456utoronto.ca ; Tel.: +1-416-946-0742; Fax: +1-416-978-8605.
                Article
                pharmaceutics-04-00104
                10.3390/pharmaceutics4010104
                3834907
                9481ab6b-ac78-43cf-b69c-a515ed36ad95
                © 2012 by the authors; licensee MDPI, Basel, Switzerland.

                This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                : 05 December 2011
                : 11 January 2012
                : 12 January 2012
                Categories
                Article

                microemulsion-based gels,gelatin,lecithin,linker microemulsions,transdermal drug delivery

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