Transdermal iontophoretic delivery of terbinafine hydrochloride: quantitation of drug levels in stratum corneum and underlying skin.
The objective of this study was to determine the effect of iontophoresis on the delivery of terbinafine hydrochloride (4%, w/w) into and across hairless rat skin. In vitro skin uptake and permeation studies were performed using Franz diffusion cells. Anodal iontophoresis was applied for 1h at current densities of 0.2, 0.3 and 0.4mA/cm(2). In addition, iontophoresis was applied for 15, 30, 45 and 60min. Studies were conducted in which the formulation was either removed or left in contact with the skin following iontophoresis and then passive delivery was assessed 23h later. Tape stripping and skin extraction were performed to quantify drug levels in the stratum corneum and the underlying skin, respectively. The samples were analyzed using HPLC. The amount of drug delivered into the stratum corneum following iontophoresis was not significantly different from the amount delivered passively (p>0.05). However, drug levels in the underlying skin were significantly higher for the iontophoretic group. The amount of terbinafine delivered into the skin layers was influenced by current density and duration of current application. Leaving the drug formulation in contact with the skin during the post-iontophoretic period had a significant effect on drug levels delivered into skin layers. Iontophoresis enhanced the delivery of terbinafine hydrochloride into the skin layers and, therefore, may be used to improve the treatment of skin fungal infections.
Sachdeva
Vishal
V
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, United States.
Siddoju
Srujana
S
Yu
Yi-Ying
YY
Kim
Hyun D
HD
Friden
Phillip M
PM
Banga
Ajay K
AK
D000279:Administration, Cutaneous; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D007478:Iontophoresis; D008297:Male; D009281:Naphthalenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010539:Permeability; D051381:Rats; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D000077291:Terbinafine; D013997:Time Factors
D000935:Antifungal Agents; D009281:Naphthalenes; D000077291:Terbinafine