Dataset Information

Stability and Formulation of Erlotinib in Skin Creams.

ABSTRACT: 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.

SUBMITTER: Nguyen D

PROVIDER: S-EPMC8839675 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature

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Stability and Formulation of Erlotinib in Skin Creams.

Nguyen David D Secrétan Philippe-Henri PH Cotteret Camille C Jacques-Gustave Emmanuelle E Greco Céline C Bodemer Christine C Schlatter Joel J Cisternino Salvatore S

Molecules (Basel, Switzerland) 20220205 3

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 ...[more]

PMID: 35164335

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Project description:Grape seeds are agro-industrial by-products, which if improperly managed, may be responsible for socioeconomic and environmental problems. Nevertheless, it is possible to effectively valorize them by means of extraction of the bioactive compounds, especially the antioxidant phenolic molecules, using a safe, green, and environmentally-friendly extractive medium (i.e., hydro-glyceric solution). In the present study, the extraction was performed using seeds from two Lebanese varieties, Obeidi and Asswad Karech, and three international varieties, Marselan, Syrah, and Cabernet Franc. The type and amount of phenolic compounds were identified by High-Performance Liquid Chromatography (HPLC). Marselan was the extract richer in catechins (132.99 ± 9.81 μg/g of dried matter), and it also contained a higher amount of phenolic compounds (49.08 ± 0.03 mg of gallic acid equivalent/g of dry matter and 10.02 ± 0.24 mg of proanthocyanidin content/g of dry matter). The antioxidant capacity of the extracts was assessed using three different colorimetric assays including 2,2-DiPhenyl-1-PicrylHydrazyl (DPPH), CUPRIC ion Reducing Antioxidant Capacity (CUPRAC), and Ferric Reducing Antioxidant Power (FRAP). As expected, Marselan exhibited the highest antioxidant activity; as well, the total phenolic and proanthocyanidin content were the highest. The stability of the Marselan extract incorporated into a commercial cream, was performed at three different temperatures (4, 25, and 50 °C), and four different concentrations (5, 4, 3, 2%), over a period of 4 months, using different methods such as centrifugation, Heat-Shock Cycles, pH, and viscosity. All Marselan hydro-glyceric extract formulations were proven to be stable over the entire 4 months, where the highest stability was achieved at 4 °C and the least at 50 °C. This study supports the suitability of the incorporation of phenolic extracts into commercial creams to enrich the cosmetic industry with effective, natural, and safe skincare products.

Dataset Information

Stability and Formulation of Erlotinib in Skin Creams.

Publications

Stability and Formulation of Erlotinib in Skin Creams.

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