Abstract
EFFECT OF THE VARIOUS PENETRATION ENHANCERS ON THE IN VITRO SKIN PERMEATION OF MELOXICAM THROUGH WHOLE RAT SKIN

Anayatollah Salimi* and Maryam Fouladi

ABSTRACT

Purpose: The main aim of this research was to investigate the effect of various penetration enhancers on the in vitro skin permeability of meloxicam. Methods: meloxicam permeability parameters through whole rat skin were studied with and without chemical penetration enhancers such as Eucalyptus oil, oleic acid and Transcutol p. Results: The skin showed barrier for meloxicam permeability through full skin and that diffusion into the skin was the rate-limiting step for drug flux. Transcutol P , eucalyptus oil and oleic acid were the most effective enhancers as they increased flux 20.7 ,16.54 and 13.54 times and diffusion coefficient 17.18,12.94 and 13.05 times in comparison with hydrated skin, respectively. Chemical penetration enhancers are materials that disrupt the lipid and lipid-protein complex structure of the skin. Two endothermic transitions were obtained at around 67 (Tm1) and 112oC (Tm2) were obtained in thermogram of hydrated whole rat skin. Tm1 and Tm2 transitions appeared to be due to melting of lipids and irreversible denaturation of intracellular keratin or melting of lipid – protein( keratin) complex ,respectively. Tm1, ΔH1 and ΔH2 were shifted by all the penetration enhancers to lower amounts in comparison with hydrated skin. Conclusion: All the chemical penetration enhancers showed markedly increase the permeation of meloxicam through whole rat skin in comparison with control.

Keywords: meloxicam, percutaneous absorption, penetration enhancers, differential scanning calorimeter.


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