Stability and Formulation of Erlotinib in Skin Creams
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 system...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-02-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/3/1070 |
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| author | David Nguyen Philippe-Henri Secrétan Camille Cotteret Emmanuelle Jacques-Gustave Céline Greco Christine Bodemer Joel Schlatter Salvatore Cisternino |
| author_facet | David Nguyen Philippe-Henri Secrétan Camille Cotteret Emmanuelle Jacques-Gustave Céline Greco Christine Bodemer Joel Schlatter Salvatore Cisternino |
| author_sort | David Nguyen |
| collection | DOAJ |
| description | 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% <i>v</i>/<i>w</i>), 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. |
| first_indexed | 2024-03-09T23:26:03Z |
| format | Article |
| id | doaj.art-1e9f0897f7724012b8fd1bd6fdacf219 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T23:26:03Z |
| publishDate | 2022-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1e9f0897f7724012b8fd1bd6fdacf2192023-11-23T17:17:07ZengMDPI AGMolecules1420-30492022-02-01273107010.3390/molecules27031070Stability and Formulation of Erlotinib in Skin CreamsDavid Nguyen0Philippe-Henri Secrétan1Camille Cotteret2Emmanuelle Jacques-Gustave3Céline Greco4Christine Bodemer5Joel Schlatter6Salvatore Cisternino7Service Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceService Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceService Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceService Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceDepartment of Pain and Palliative Care Unit, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceIMAGINE Institute, INSERM, U1163, Université de Paris, F-75015 Paris, FranceService Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceService Pharmacie, APHP, Hôpital Necker-Enfants Malades, F-75015 Paris, FranceRecent 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% <i>v</i>/<i>w</i>), 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.https://www.mdpi.com/1420-3049/27/3/1070dermatologydrug repurposingerlotinibrare diseasestability indicatingOlmsted |
| spellingShingle | David Nguyen Philippe-Henri Secrétan Camille Cotteret Emmanuelle Jacques-Gustave Céline Greco Christine Bodemer Joel Schlatter Salvatore Cisternino Stability and Formulation of Erlotinib in Skin Creams Molecules dermatology drug repurposing erlotinib rare disease stability indicating Olmsted |
| title | Stability and Formulation of Erlotinib in Skin Creams |
| title_full | Stability and Formulation of Erlotinib in Skin Creams |
| title_fullStr | Stability and Formulation of Erlotinib in Skin Creams |
| title_full_unstemmed | Stability and Formulation of Erlotinib in Skin Creams |
| title_short | Stability and Formulation of Erlotinib in Skin Creams |
| title_sort | stability and formulation of erlotinib in skin creams |
| topic | dermatology drug repurposing erlotinib rare disease stability indicating Olmsted |
| url | https://www.mdpi.com/1420-3049/27/3/1070 |
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