Influence of electrical and chemical factors on transdermal iontophoretic delivery of three diclofenac salts.
The aim of this present study was to investigate the in vitro transdermal iontophoretic delivery of three diclofenac salts--diclofenac sodium (DFS), diclofenac potassium (DFP), and diclofenac diethylammonium (DFD). A series of physicochemical and electrical variables which might affect iontophoretic permeation of diclofenac salts was studied. Application of 0.3 mA/cm2 current density significantly increased the transdermal flux of diclofenac salts as compared to passive transport. The iontophoretic enhancement increased in the order of DFS>DFP>DFD. The permeability coefficient of diclofenac salts all decreased with increasing donor concentration during iontophoresis. The addition of buffer ions and salt ions such as NaCl, KCl, and C4H12ClN reduced the permeation of diclofenac salts due to competition. However, this effect was lesser for DFD than for DFS and DFP. Comparing the various application modes of iontophoresis, the discontinuous on/off mode showed lower but more constant flux than the continuous mode.
Fang
J Y
JY
School of Pharmacy, Kaohsiung Medical University, Taiwan.
Wang
R J
RJ
Huang
Y B
YB
Wu
P C
PC
Tsai
Y H
YH
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D005260:Female; D066298:In Vitro Techniques; D007478:Iontophoresis; D051379:Mice; D008819:Mice, Nude; D014677:Pharmaceutical Vehicles; D013056:Spectrophotometry, Ultraviolet
D000894:Anti-Inflammatory Agents, Non-Steroidal; D014677:Pharmaceutical Vehicles; D004008:Diclofenac