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Impact of Menthol Concentration on Ketoprofen Permeation and Photostability in Compounded Topical Preparations in a
Urszula Adamiak-Giera1, Michał Gackowski2,3, Damian Malinowski1
1Department of Pharmacokinetics and Therapeutic Drug Monitoring, Pomeranian Medical University in Szczecin, Szczecin 70-111, Poland.
Background:
Topical nonsteroidal anti-inflammatory drugs provide localized pain relief while reducing the risk of systemic adverse effects. Menthol is frequently used in topical formulations both as an analgesic agent and as a penetration enhancer.
Objective:
This study evaluated the effect of menthol concentration on ketoprofen permeation through Strat-M membranes and photostability in compounded topical formulations based on a Pentravan vehicle.
Research Design And Methods:
Semisolid formulations containing ketoprofen, lidocaine hydrochloride, and increasing concentrations of menthol were prepared using the Pentravan base. In vitro permeation experiments were performed using Franz diffusion cells with Strat-M membranes as a screening model. Ketoprofen concentrations were determined using UHPLC analysis. Photostability under UVA exposure (0-200 Wh/m2) was also assessed.
Results:
Ketoprofen permeation increased with increasing menthol concentration. After 12 h, the cumulative amount detected in the acceptor phase ranged from 194.9 μg for the menthol-free formulation to 475.9 μg for the formulation containing 10% menthol. Photostability studies showed formulation-dependent degradation profiles. The menthol-free formulation retained the highest proportion of ketoprofen during UVA exposure, whereas the menthol-containing formulation and the commercial product showed more pronounced drug degradation.
Conclusion:
Menthol enhanced ketoprofen permeation in the applied in vitro model while also influencing the drug's photodegradation behavior under UVA exposure, highlighting the importance of formulation composition in compounded topical preparations.
Insights
Menthol increases topical ketoprofen permeation in formulations but may affect drug stability under UVA light. This highlights the importance of menthol concentration in compounded topical preparations.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Drug Delivery Systems
Background:
- Topical nonsteroidal anti-inflammatory drugs (NSAIDs) offer localized pain relief with fewer systemic side effects.
- Menthol is commonly incorporated into topical products for its analgesic properties and ability to enhance drug penetration.
Purpose of the Study:
- To investigate how varying menthol concentrations impact ketoprofen permeation through Strat-M membranes.
- To assess the photostability of ketoprofen in compounded topical formulations containing different menthol levels.
Main Methods:
- Semisolid formulations with ketoprofen, lidocaine hydrochloride, and increasing menthol concentrations were prepared using a Pentravan vehicle.
- In vitro permeation studies utilized Franz diffusion cells with Strat-M membranes.
- Ketoprofen levels were quantified via UHPLC, and photostability was evaluated under UVA irradiation.
Main Results:
- Ketoprofen permeation significantly increased with higher menthol concentrations.
- Formulations with 10% menthol showed higher ketoprofen permeation compared to menthol-free ones.
- Menthol influenced ketoprofen's photodegradation; menthol-free formulations were more stable under UVA exposure.
Conclusions:
- Menthol acts as a penetration enhancer for ketoprofen in topical formulations.
- The concentration of menthol affects both drug permeation and photostability.
- Formulation composition is critical for the efficacy and stability of compounded topical medications.
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