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ACTA Pharmaceutica Sciencia
2008 , Vol 50 , Num 3
EFFECT OF TERPENES AS PENETRATION ENHANCERS ON PERCUTANEOUS PENETRATION OF TIAPROFENIC ACID THROUGH PIG SKIN
Istanbul University, Faculty of Pharmacy Department of Pharmacology,Beyazit- Istanbul-Turkey
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Tiaprofenic acid (TA) a nonsteroidal antiinflammatory agent that lipophilic character and widely used in rheumatoid arthritis via oral route. TA has various side-effects like other prostaglandine inhibitors in gastrointestinal system and these effects limit its use e.g., active stomach ulcer patients. Hence, local application of the drug as important as systemic application such cases mentioned above. The influence of different type terpenes in various combinations on percutaneous penetration of TA from Carbopol® 940 based gel formulations was investigated using Franz-type diffusion cells and pig skin. Four types of terpenes such as nerolidol, d-limonene, eucalyptol and menthol were employed as penetration enhancers and the steady-state flux, the lag time and permeability coefficients of TA for each formulation were calculated. The results of permeation studies showed that the rank order of enhancement ratio (ERflux) for TA was d-limonene (5.89) > eucalyptol (4.73) > menthol (3.69) > nerolidol (1.43). Amongst the used terpenes in the gel formulations, d-limonene and eucalyptol were found to be an effective penetration enhancer for TA. However, further in vivo penetration studies should be performed to show the validity of the results of ex vivo penetration studies and to determine the therapeutic level of the drug.
Keywords :
TIAPROFENIC ACID, TERPENES, PERCUTANEOUS PENETRATION, PIG SKIN, CARBOPOL® 940