Development and evaluation on transdermal delivery of enoxacin via chemical enhancers and physical iontophoresis.
Iontophoresis and enhancers were performed to enhance percutaneous absorption of enoxacin so as to compare the enhancement between these two enhancing methods. The cationic surfactant of benzalkonium chloride showed the highest enhancing activity for enoxacin for all pH values of buffer vehicles. The enhancement factor of sodium laurylsulfate showed a dose-dependent property between the range of 0.1% to 3.0% concentration. Nonionic surfactant of Polysorbate 80 did not exhibit any enhancing effect on the percutaneous absorption of enoxacin. The highest enhancement factor of iontophoretic delivery was observed at pH 5.0 solution of anodal iontophoresis for cationic enoxacin. The cathodal iontophoresis of negative molecules and anodal iontophoresis of neutral molecules showed lower enhancing effect for enoxacin. The fact that the skin residuals of enoxacin after iontophoresis showed both tremendous and current density-dependent amounts for cationic enoxacin suggested local skin and soft tissue infections might be treated by this physical enhancement method. Combination of benzalkonium chloride and iontophoresis exerted a synergistic effect for anionic enoxacin in pH 10.0, which was possibly due to the shielding of negative charge in skin and the water molecules carried by chloride.
School of Pharmacy, Chia Nan College of Pharmacy and Science, Tainan Hsien, Taiwan, ROC.
J Y
JY
Fang
H H
HH
Lin
H I
HI
Chen
Y H
YH
Tsai
D000279:Administration, Cutaneous; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D015365:Enoxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005079:Excipients; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007478:Iontophoresis; D014677:Pharmaceutical Vehicles; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013268:Stimulation, Chemical; D013501:Surface-Active Agents / Q000494:pharmacology
D000890:Anti-Infective Agents; D005079:Excipients; D014677:Pharmaceutical Vehicles; D013501:Surface-Active Agents; D015365:Enoxacin