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. 2014 Mar 30;7(4):E39–E45. doi: 10.1208/pt070488

Transdermal delivery of diclofenac sodium through rat skin from various formulations

Işik Sarigüllü Özgüney 1,✉, Hatice Yeşim Karasulu 1, Gülten Kantarci 2, Sumru Sözer 3, Tamer Güneri 1, Gökhan Ertan 1
PMCID: PMC2750325  PMID: 16796357

Abstract

The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro potential of these formulations, permeation studies were performed with Franz diffusion cells using excised dorsal rat skin. To investigate their in vivo performance, a carrageenan-induced rat paw edema model was used. The commercial formulation of DS (C) was used as a reference formulation. The results of the in vitro permeation studies and the paw edema tests were analyzed by repeated-measures analysis of variance. The in vitro permeation studies found that M was superior to G and C and that adding DMSO to M increased the permeation rate. The permeability coefficients (Kp) of DS from M and M+DMSO were higher (Kp=4.9×10−3±3.6×10−4 cm/h and 5.3×10−3±1.2×10−3 cm/h, respectively) than the Kp of DS from C (Kp=2.7×10−3±7.3×10−4 cm/h) and G (Kp=4.5×10−3±4.5×10−5 cm/h). In the paw edema test, M showed the best permeation and effectiveness, and M+DMSO had nearly the same effect as M. The in vitro and in vivo studies showed that M could be a new, alternative dosage form for effective therapy.

Keywords: microemulsion, diclofenac sodium, in vitro permeation, carrageenan-induced rat paw edema test

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