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Nanostructured Lipid Carrier Gel for the Dermal Application of Lidocaine: Comparison of Skin Penetration Testing Methods

1
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, 6720 Szeged, Hungary
2
Frederic and Mary Wolfe Center, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, Toledo, OH 43614, USA
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(7), 310; https://doi.org/10.3390/pharmaceutics11070310
Received: 6 May 2019 / Revised: 18 June 2019 / Accepted: 25 June 2019 / Published: 2 July 2019
(This article belongs to the Special Issue Semisolid Dosage)
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Abstract

The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured lipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test the penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin penetration modeling methods. The formulations were characterized by laser diffraction, rheological measurements and microscopic examinations. Various in vitro methods were used to study drug release, diffusion and penetration. Two types of vertical Franz diffusion cells with three different membranes, including cellulose, Strat-M®, and heat separated human epidermis were used and compared to the Skin-parallel artificial membrane permeability assay (PAMPA) method. Results indicated that the nanostructured lipid carrier dispersion had to be gelified as soon as possible for proper stability. Both the Skin-PAMPA model and Strat-M® membranes correlated favorably with heat separated human epidermis in this research, with the Strat-M® membranes sharing the most similar drug permeability profile to an ex vivo human skin model. Our experimental findings suggest that even when the best available in vitro experiment is selected for modeling human skin penetration to study nanostructured lipid carrier gel systems, relevant in vitro/in vivo correlation should be made to calculate the drug release/permeation in vivo. Future investigations in this field are still needed to demonstrate the influence of membranes and equipment from other classes on other drug candidates. View Full-Text
Keywords: dermal drug delivery; diffusion cell; Franz diffusion; Skin-PAMPA; Strat-M® membrane; nanocarrier dermal drug delivery; diffusion cell; Franz diffusion; Skin-PAMPA; Strat-M® membrane; nanocarrier
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Zsikó, S.; Cutcher, K.; Kovács, A.; Budai-Szűcs, M.; Gácsi, A.; Baki, G.; Csányi, E.; Berkó, S. Nanostructured Lipid Carrier Gel for the Dermal Application of Lidocaine: Comparison of Skin Penetration Testing Methods. Pharmaceutics 2019, 11, 310.

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