Transdermal delivery of diclofenac sodium through rat skin from various formulations.
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 x 10(-3) +/- 3.6 x 10(-4) cm/h and 5.3 x 10(-3) +/- 1.2 x 10(-3) cm/h, respectively) than the Kp of DS from C (Kp = 2.7 x 10(-3) +/- 7.3 x 10(-4) cm/h) and G (Kp = 4.5 x 10(-3) +/- 4.5 x 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.
Sarigüllü Ozgüney
Işik
I
Faculty of Pharmacy, University of Ege, Department of Pharmaceutical Technology, 35100 Bornova, Izmir, Turkey. isik.ozguney@ege.edu.tr
Yeşim Karasulu
Hatice
H
Kantarci
Gülten
G
Sözer
Sumru
S
Güneri
Tamer
T
Ertan
Gökhan
G
D000042:Absorption; D000279:Administration, Cutaneous; D000818:Animals; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry*; D004058:Diffusion; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D066298:In Vitro Techniques; D008297:Male; D008422:Materials Testing; D051381:Rats; D012867:Skin / Q000737:chemistry*; D012869:Skin Absorption
D004337:Drug Carriers; D005079:Excipients; D004008:Diclofenac