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Titel: Tofacitinib Loaded Squalenyl Nanoparticles for Targeted Follicular Delivery in Inflammatory Skin Diseases
VerfasserIn: Christmann, Rebekka
Ho, Duy-Khiet
Wilzopolski, Jenny
Lee, Sangeun
Koch, Marcus
Loretz, Brigitta
Vogt, Thomas
Bäumer, Wolfgang
Schaefer, Ulrich F.
Lehr, Claus-Michael
Sprache: Englisch
Titel: Pharmaceutics
Bandnummer: 12
Heft: 12
Verlag/Plattform: MDPI
Erscheinungsjahr: 2020
Freie Schlagwörter: targeted drug delivery
hair follicle
in vivo allergic dermatitis mouse model
follicular delivery
interfollicular delivery
nanoparticles
squalene
DDC-Sachgruppe: 500 Naturwissenschaften
600 Technik
Dokumenttyp: Journalartikel / Zeitschriftenartikel
Abstract: Tofacitinib (TFB), a Janus kinase inhibitor, has shown excellent success off-label in treating various dermatological diseases, especially alopecia areata (AA). However, TFB’s safe and targeted delivery into hair follicles (HFs) is highly desirable due to its systemic adverse effects. Nanoparticles (NPs) can enhance targeted follicular drug delivery and minimize interfollicular permeation and thereby reduce systemic drug exposure. In this study, we report a facile method to assemble the stable and uniform 240 nm TFB loaded squalenyl derivative (SqD) nanoparticles (TFB SqD NPs) in aqueous solution, which allowed an excellent loading capacity (LC) of 20%. The SqD NPs showed an enhanced TFB delivery into HFs compared to the aqueous formulations of plain drug in an ex vivo pig ear model. Furthermore, the therapeutic efficacy of the TFB SqD NPs was studied in a mouse model of allergic dermatitis by ear swelling reduction and compared to TFB dissolved in a non-aqueous mixture of acetone and DMSO (7:1 v/v). Whereas such formulation would not be acceptable for use in the clinic, the TFB SqD NPs dispersed in water illustrated a better reduction in inflammatory effects than plain TFB’s aqueous formulation, implying both encouraging good in vivo efficacy and safety. These findings support the potential of TFB SqD NPs for developing a long-term topical therapy of AA.
DOI der Erstveröffentlichung: 10.3390/pharmaceutics12121131
Link zu diesem Datensatz: urn:nbn:de:bsz:291--ds-329666
hdl:20.500.11880/30315
http://dx.doi.org/10.22028/D291-32966
ISSN: 1999-4923
Datum des Eintrags: 6-Jan-2021
Bezeichnung des in Beziehung stehenden Objekts: Supplementary Materials
In Beziehung stehendes Objekt: https://www.mdpi.com/1999-4923/12/12/1131/s1
Fakultät: M - Medizinische Fakultät
NT - Naturwissenschaftlich- Technische Fakultät
Fachrichtung: M - Dermatologie
NT - Pharmazie
Professur: M - Prof. Dr. Thomas Vogt
NT - Prof. Dr. Claus-Michael Lehr
Sammlung:SciDok - Der Wissenschaftsserver der Universität des Saarlandes

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