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Dermal Delivery of the High-Molecular-Weight Drug Tacrolimus by Means of Polyglycerol-Based Nanogels

1
Clinical Research Center for Hair and Skin Science, Department of Dermatology and Allergy, Charité—Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, 10117 Berlin, Germany
2
Institut für Chemie und Biochemie, Freie Universität Berlin, 14195 Berlin, Germany
3
Institute of Nutritional Science, Department of Nutritional Toxicology, University of Potsdam, 14558 Nuthetal, Germany
4
Department of Molecular Biology, University of Duisburg-Essen, 45147 Essen, Germany
5
POLYMAT and Applied Chemistry Department, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel de Lardizabal 3, 20018 Donostia-San Sebastián, Spain
6
IKERBASQUE, Basque Foundation for Science, 48013 Bilbao, Spain
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(8), 394; https://doi.org/10.3390/pharmaceutics11080394
Received: 30 June 2019 / Revised: 29 July 2019 / Accepted: 31 July 2019 / Published: 5 August 2019
(This article belongs to the Special Issue Semisolid Dosage)
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Abstract

Polyglycerol-based thermoresponsive nanogels (tNGs) have been shown to have excellent skin hydration properties and to be valuable delivery systems for sustained release of drugs into skin. In this study, we compared the skin penetration of tacrolimus formulated in tNGs with a commercial 0.1% tacrolimus ointment. The penetration of the drug was investigated in ex vivo abdominal and breast skin, while different methods for skin barrier disruption were investigated to improve skin permeability or simulate inflammatory conditions with compromised skin barrier. The amount of penetrated tacrolimus was measured in skin extracts by liquid chromatography tandem-mass spectrometry (LC-MS/MS), whereas the inflammatory markers IL-6 and IL-8 were detected by enzyme-linked immunosorbent assay (ELISA). Higher amounts of tacrolimus penetrated in breast as compared to abdominal skin or in barrier-disrupted as compared to intact skin, confirming that the stratum corneum is the main barrier for tacrolimus skin penetration. The anti-proliferative effect of the penetrated drug was measured in skin tissue/Jurkat cells co-cultures. Interestingly, tNGs exhibited similar anti-proliferative effects as the 0.1% tacrolimus ointment. We conclude that polyglycerol-based nanogels represent an interesting alternative to paraffin-based formulations for the treatment of inflammatory skin conditions. View Full-Text
Keywords: tacrolimus formulation; nanogels; skin penetration; drug delivery; human excised skin; Jurkat cells tacrolimus formulation; nanogels; skin penetration; drug delivery; human excised skin; Jurkat cells
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Rancan, F.; Volkmann, H.; Giulbudagian, M.; Schumacher, F.; Stanko, J.I.; Kleuser, B.; Blume-Peytavi, U.; Calderón, M.; Vogt, A. Dermal Delivery of the High-Molecular-Weight Drug Tacrolimus by Means of Polyglycerol-Based Nanogels. Pharmaceutics 2019, 11, 394.

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