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Communication

Stability and Formulation of Erlotinib in Skin Creams

1
Service Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, France
2
Matériaux et santé, Université Paris-Saclay, F-92296 Châtenay-Malabry, France
3
Department of Pain and Palliative Care Unit, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, France
4
IMAGINE Institute, INSERM, U1163, Université de Paris, F-75015 Paris, France
5
Reference Center for Genodermatoses (MAGEC), Department of Dermatology, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, France
6
Pharmacie, APHP, Hôpital Paul-Doumer, F-60140 Liancourt, France
7
INSERM UMR_S1144, Optimisation Thérapeutique en Neuropsychopharmacologie, Université de Paris, F-75006 Paris, France
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
These authors contributed equally to this work.
Academic Editors: Dániel Nemes and Ildikó Bácskay
Molecules 2022, 27(3), 1070; https://doi.org/10.3390/molecules27031070
Received: 16 January 2022 / Revised: 2 February 2022 / Accepted: 3 February 2022 / Published: 5 February 2022
Recent studies have highlighted the benefit of repurposing oral erlotinib (ERL) treatment in some rare skin diseases such as Olmsted syndrome. The use of a topical ERL skin treatment instead of the currently available ERL tablets may be appealing to treat skin disorders while reducing adverse systemic effects and exposure. A method to prepare 0.2% ERL cream, without resorting to a pure active pharmaceutical ingredient, was developed and the formulation was optimized to improve ERL stability over time. Erlotinib extraction from tablets was incomplete with Transcutol, whereas dimethyl sulfoxide (DMSO) allowed 100% erlotinib recovery. During preliminary studies, ERL was shown to be sensitive to oxidation and acidic pH in solution and when added to selected creams (i.e., Excipial, Nourivan Antiox, Pentravan, and Versatile). The results also showed that use of DMSO (5% v/w), neutral pH, as well as a topical agent containing antioxidant substances (Nourivan Antiox) were key factors to maintain the initial erlotinib concentration. The proposed ERL cream formulation at neutral pH contains a homogeneous amount of ERL and is stable for at least 42 days at room temperature in Nourivan cream with antioxidant properties. View Full-Text
Keywords: dermatology; drug repurposing; erlotinib; rare disease; stability indicating; Olmsted; skin cancer; topical dermatology; drug repurposing; erlotinib; rare disease; stability indicating; Olmsted; skin cancer; topical
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MDPI and ACS Style

Nguyen, D.; Secrétan, P.-H.; Cotteret, C.; Jacques-Gustave, E.; Greco, C.; Bodemer, C.; Schlatter, J.; Cisternino, S. Stability and Formulation of Erlotinib in Skin Creams. Molecules 2022, 27, 1070. https://doi.org/10.3390/molecules27031070

AMA Style

Nguyen D, Secrétan P-H, Cotteret C, Jacques-Gustave E, Greco C, Bodemer C, Schlatter J, Cisternino S. Stability and Formulation of Erlotinib in Skin Creams. Molecules. 2022; 27(3):1070. https://doi.org/10.3390/molecules27031070

Chicago/Turabian Style

Nguyen, David, Philippe-Henri Secrétan, Camille Cotteret, Emmanuelle Jacques-Gustave, Céline Greco, Christine Bodemer, Joel Schlatter, and Salvatore Cisternino. 2022. "Stability and Formulation of Erlotinib in Skin Creams" Molecules 27, no. 3: 1070. https://doi.org/10.3390/molecules27031070

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