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In vitro evaluation of nimodipine permeation through human epidermis using response surface methodology.
S A Giannakou1, P P Dallas, D M Rekkas
1School of Pharmacy, Department of Pharmaceutical Technology, University of Athens, Panepistimiopolis, Zografou, 15771, Athens, Greece.
International Journal of Pharmaceutics
|June 28, 2002
Summary
This study explored how caprylic acid and cineol enhance nimodipine permeation through skin. Caprylic acid was key initially, but the combination proved most effective over time for improved drug delivery.
Area of Science:
- Pharmacology and Pharmaceutics
- Dermal Drug Delivery
- Enhancer Technology
Background:
- Nimodipine is a calcium channel blocker used for subarachnoid hemorrhage.
- Enhancing transdermal drug permeation is crucial for effective topical and systemic delivery.
- Understanding enhancer combinations can optimize drug formulations.
Purpose of the Study:
- To investigate the combined effect of caprylic acid and cineol on nimodipine permeation through human cadaver epidermis.
- To determine the optimal concentrations of these enhancers for maximizing nimodipine delivery.
- To elucidate the time-dependent role of each enhancer in the permeation process.
Main Methods:
- Utilized the response surface method, a quadratic optimization technique.
- Investigated nimodipine permeation through human cadaver epidermis over 24, 48, and 72 hours.
- Analyzed the impact of varying concentrations of caprylic acid and cineol.
Main Results:
- Caprylic acid significantly increased nimodipine permeation at 24 hours.
- The combination of caprylic acid and cineol enhanced permeation at 48 and 72 hours.
- Optimal permeation was achieved with cineol concentrations between 3.0-5.0% (v/v) and caprylic acid between 8.0-9.5% (v/v).
Conclusions:
- The synergistic effect of caprylic acid and cineol is time-dependent for nimodipine permeation.
- Optimized enhancer concentrations are critical for maximizing transdermal drug delivery.
- This study provides valuable insights for developing effective nimodipine topical formulations.