Abstract
BackgroundRubbing a topical NSAID (non steroidal anti-inflammatory drug) on the skin may increase local drug permeation, affecting its distribution to the site of pain and inflammation. The present study evaluates this hypothesis, by assessing in vitro the effect on skin permeation of applying diclofenac-dieythylamine 1.16% gel with or without rubbing.MethodsA single dose of 5 mg/cm2 diclofenac-diethylamine 1.16% gel was applied on excised human skin mounted in Franz-type diffusion cells without or with rubbing for 45 s. Drug penetration into the skin layers was determined after 1 h using the tape stripping technique. In vitro cutaneous permeation into the receptor fluid of the diffusion chamber was measured up to 24 h. Skin electrical resistance was also recorded.ResultsApplication of diclofenac-diethylamine 1.16% gel with rubbing resulted to a 5-fold higher flux of diclofenac through the skin than when applied without rubbing at 8 h (P = 0.04). Skin rubbing for 45 s decreased by 2-fold skin electrical resistance when compared to the standard application. Application of diclofenac-diethylamine 1.16% gel with rubbing tended to result in higher accumulation in the stripped skin vs. the superficial skin layers when applied without rubbing (P = 0.2).ConclusionThese results suggest that rubbing may alter the superficial skin layer resulting in a transient faster initial diffusion of topically applied diclofenac through the stratum corneum into the deeper skin layer of the dermis to the tissue target.
Highlights
Rubbing a topical non-steroidal anti-inflammatory drug (NSAID) on the skin may increase local drug permeation, affecting its distribution to the site of pain and inflammation
There is a common perception that the act of rubbing/ massaging a topical NSAID on the site of pain may provide an additional benefit to the patient
We sought to assess the hypothesis that rubbing a topical NSAID onto the skin may result in increased penetration of the drug through the skin layer and affecting the availability of the active ingredient in subcutaneous tissues
Summary
Rubbing a topical NSAID (non steroidal anti-inflammatory drug) on the skin may increase local drug permeation, affecting its distribution to the site of pain and inflammation. The mechanisms by which the act of rubbing may affect the efficacy of the drug are not clear and they have not being investigated extensively, but they may involve the activation of gating mechanisms and the desensitization of local nerve endings. With this present study, we sought to assess the hypothesis that rubbing a topical NSAID onto the skin may result in increased penetration of the drug through the skin layer and affecting the availability of the active ingredient in subcutaneous tissues. The present study compared the in vitro skin permeation and distribution of 1.16% diclofenac-diethylamine gel after application without or with a rubbing for 45 s
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