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dc.contributor.authorRancan, Fiorenza
dc.contributor.authorVolkmann, Hildburg
dc.contributor.authorGiulbudagian, Michael
dc.contributor.authorSchumacher, Fabian
dc.contributor.authorStanko, Jessica Isolde
dc.contributor.authorKleuser, Burkhard
dc.contributor.authorBlume Peytavi, Ulrike
dc.contributor.authorCalderón, Marcelo
dc.contributor.authorVogt, Annika
dc.date.accessioned2020-01-15T13:38:52Z
dc.date.available2020-01-15T13:38:52Z
dc.date.issued2019-08
dc.identifier.citationPharmaceutics 11(8) : (2019) // Article ID 394es_ES
dc.identifier.issn1999-4923
dc.identifier.urihttp://hdl.handle.net/10810/38477
dc.description.abstractPolyglycerol-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.es_ES
dc.description.sponsorshipThis research was funded by the German Research Foundation (DFG), grant SFB1112, projects C04, A04, and Z0. We also acknowledge support from the German Research Foundation (DFG) and the Open Access Publication Fund of Charite-Universitatsmedizin Berlin for publication costs.es_ES
dc.language.isoenges_ES
dc.publisherMDPIes_ES
dc.rightsinfo:eu-repo/semantics/openAccesses_ES
dc.rights.urihttp://creativecommons.org/licenses/by/3.0/es/*
dc.subjecttacrolimus formulationes_ES
dc.subjectnanogelses_ES
dc.subjectskin penetrationes_ES
dc.subjectdrug deliveryes_ES
dc.subjecthuman excised skines_ES
dc.subjectthermoresponsive nanogelses_ES
dc.subjecthuman skines_ES
dc.subjectpart IIes_ES
dc.subjecttopical deliveryes_ES
dc.subjecthair-follicleses_ES
dc.subjectcyclosporine-aes_ES
dc.subjectfk506es_ES
dc.subjectmechanismses_ES
dc.subjectbarrieres_ES
dc.subjectpenetrationes_ES
dc.titleDermal Delivery of the High-Molecular-Weight Drug Tacrolimus by Means of Polyglycerol-Based Nanogelses_ES
dc.typeinfo:eu-repo/semantics/articlees_ES
dc.rights.holderThis 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 citedes_ES
dc.rights.holderAtribución 3.0 España*
dc.relation.publisherversionhttps://www.mdpi.com/1999-4923/11/8/394es_ES
dc.identifier.doi10.3390/pharmaceutics11080394
dc.departamentoesBioquímica y biología moleculares_ES
dc.departamentoeuBiokimika eta biologia molekularraes_ES


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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
Except where otherwise noted, this item's license is described as 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