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Tofacitinib loaded squalenyl nanoparticles for targeted follicular delivery in inflammatory skin diseases

  • 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.

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Document Type:Article
Author:Rebekka ChristmannORCiD, Duy-Khiet HoORCiD, Jenny Wilzopolski, Sangeun Lee, Marcus Koch, Brigitta LoretzORCiD, Thomas Vogt, Wolfgang Bäumer, Ulrich F. Schaefer, Claus-Michael LehrORCiD
Parent Title (English):Pharmaceutics
First Page:1131
Last Page:1-17
Year of first Publication:2020
Release Date:2022/11/18
Tag:follicular delivery; hair follicle; interfollicular delivery; invivo allergic dermatitis mous model; nanoparticles; squalene; targeted drug delivery
Impact:06.321 (2020)
Scientific Units:Physical Analytics
Open Access:Open Access
Signature:INM 2020/129
Licence (German):License LogoCreative Commons - CC BY - Namensnennung 4.0 International