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Diclofenac concentrations in defined tissue layers after topical administration
M Müller1, H Mascher, C Kikuta
1Department of Clinical Pharmacology, University of Vienna, Währinger Gürtel, Austria.
Clinical Pharmacology and Therapeutics
|October 23, 1997
Summary
Topical diclofenac penetration into skin tissues is unpredictable after single doses. Individual skin properties significantly influence how much nonsteroidal anti-inflammatory drug reaches target areas.
Area of Science:
- Pharmacology
- Dermatology
- Drug Delivery
Background:
- Therapeutic concentrations of topical nonsteroidal anti-inflammatory drugs (NSAIDs) in target tissues remain unclear.
- This study investigates diclofenac concentrations in skin layers following topical application.
Purpose of the Study:
- To measure diclofenac concentrations in superficial and deep skin layers using in vivo microdialysis.
- To assess the relationship between drug concentration and depth of tissue penetration.
Main Methods:
- In vivo microdialysis probes inserted into superficial (3.9 mm) and deep (9.3 mm) tissue layers in 20 healthy volunteers.
- Skin-to-probe tip distance measured by ultrasound; topical diclofenac (300 mg/100 cm2) applied.
- Concentration-time profiles monitored for 5 hours.
Main Results:
- Concentration-time profiles successfully obtained in 11 of 20 experiments.
- No correlation found between area under the concentration-time curve (AUC) and probe insertion depth.
- Mean AUC for superficial layers was 532 ± 197 μg·min/mL; for deep layers, it was 438 ± 249 μg·min/mL.
Conclusions:
- Transdermal penetration of diclofenac after single doses is not predictable.
- Individual skin properties appear to significantly influence diclofenac absorption and distribution.