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Transcutaneous absorption of naproxen gel
F A van den Ouweland1, P C Eenhoorn, Y Tan
1Department of Medicine, University Hospital Sint Radboud, Nijmegen, The Netherlands.
European Journal of Clinical Pharmacology
|January 1, 1989
Summary
Topical naproxen gel applied to the skin showed low bioavailability in healthy volunteers. Despite minimal absorption, localized drug accumulation may suggest a potential pharmacological effect.
Area of Science:
- Pharmacology
- Dermatology
- Pharmacokinetics
Background:
- Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) commonly used for pain and inflammation.
- Topical drug delivery offers localized treatment with potentially reduced systemic side effects.
- Understanding the pharmacokinetics of topical naproxen is crucial for optimizing its therapeutic use.
Purpose of the Study:
- To investigate the pharmacokinetics and bioavailability of naproxen following cutaneous application of topical gels.
- To determine the extent of naproxen absorption and its elimination pathways after topical administration.
Main Methods:
- Healthy volunteers received topical naproxen gels at 5% and 10% concentrations.
- Serum naproxen concentrations and cumulative urinary metabolite excretion were measured up to 96 hours post-application.
- Bioavailability was calculated using both serum and urine data.
Main Results:
- Mean bioavailability was low, ranging from 1.0% to 2.1% depending on gel concentration and measurement method (serum or urine).
- The 5% gel resulted in slightly higher bioavailability compared to the 10% gel.
- Serum concentration-time curves suggested potential cutaneous accumulation of naproxen.
Conclusions:
- Topical naproxen gels exhibit limited systemic absorption in healthy volunteers.
- The observed cutaneous accumulation warrants further investigation for potential localized pharmacological effects.
- Topical naproxen may offer a localized anti-inflammatory option with minimal systemic exposure.