Effect of cyclosporine A – Tempol topical gel for the treatment of alopecia and anti-inflammatory disorders

Over the years, extensive research has been carried out to develop new chemical entities for hair loss treatment. Despite these efforts, the newly developed topical and oral treatments have not proven to be curative. Hair loss can result from underlying mechanisms, such as inflammation and apoptosis around hair follicles. We have developed a nanoemulsion based on Pemulen gel for topical application, tentatively addressing both mechanisms. The novel formulation contains two well-known molecules: Cyclosporin A (CsA), an immunosuppressant calcineurin inhibitor, and Tempol, a potent antioxidant. The in vitro permeation study on human skin revealed that the CsA-Tempol gel formulation effectively delivered CsA into the skin’s inner target layer, the dermis.

The effects of the CsA-Tempol gel on hair regrowth were further demonstrated in the in vivo well-established androgenetic model induced in female C57BL/6 mice. The beneficial outcome was statistically confirmed by quantitative analysis of hair regrowth, weasured by color density. The results were further supported by histology analysis. Our findings revealed a topical synergy effect, resulting in lower therapeutic concentrations of both actives unlikely to cause systemic side effects. Overall, our research suggests that the CsA-Tempol gel is a highly promising platform for treating alopecia.

Materials

CsA was graciously provided by Teva (Opava, Komarov, Czech Republic). Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl), Tween 80 (polyoxyethylene (80) sorbitan monooleate), MTT (3-(4,5 dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide), DNFB (1-Fluoro-2,4-dinitrobenzene) and DHT (5α-androstane-3β,17β-diol) were purchased from Sigma-Aldrich (Rehovot, Israel). [3H]-CsA was purchased from ARC Ameican Radiolabeled Chemicals, Inc (St. Louis, MO, USA).

Sarin Palakkal, Angèle Cortial, Marina Frušić-Zlotkin, Yoram Soroka, Tomer Tzur, Taher Nassar, Simon Benita, Effect of cyclosporine A – Tempol topical gel for the treatment of alopecia and anti-inflammatory disorders, International Journal of Pharmaceutics, 2023, 123121, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2023.123121.

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