Effect of polyethylene glycols on the trans-ungual delivery of terbinafine.
Topical nail drug delivery could be improved by identifying potent chemical penetration enhancers. The purpose of this study was to assess the effect of polyethylene glycols (PEGs) on the trans-ungual delivery of terbinafine. In vitro permeation studies were carried out by passive and iontophoresis (0.5 mA/cm2) processes for a period of 1 h using gel formulations containing different molecular weight PEGs (30%w/w). The release of drug from the loaded nail plates and the possible mechanisms for the enhanced delivery was studied. Passive delivery using formulation with low molecular weight PEGs (200 and 400 MW) indicated moderate enhancement in the permeation and drug load in the nail plate, compared to the control formulation. However, the effect of low molecular weight PEGs was predominant during iontophoresis process with greater amount of terbinafine being permeated (≈35 µg/cm2) and loaded into the nail plate (≈2.7 µg/mg). However, little or no effect on drug delivery was observed with high molecular weight PEGs (1000- 3350 MW) in passive and iontophoresis processes. Release of drug from the nail plates loaded by iontophoresis using low molecular weight PEG (400 MW) exhibited sustain effect which continued over a period of 72 days. The enhancement in drug permeation by low molecular weight PEGs is likely due to their ability to lead to greater water uptake and swelling of nail. This study concluded that the low molecular weight PEGs are indeed a promising trans-ungual permeation enhancer.
Department of Pharmaceutics, The University of Mississippi, University, MS 38677, USA.
Anroop B
AB
Nair
Bireswar
B
Chakraborty
S Narasimha
SN
Murthy
D000042:Absorption / Q000187:drug effects; D000277:Adjuvants, Pharmaceutic / Q000494:pharmacology*; D000287:Administration, Topical; D000368:Aged; D000369:Aged, 80 and over; D000935:Antifungal Agents / Q000008:administration & dosage / Q000378:metabolism; D004058:Diffusion; D006801:Humans; D066298:In Vitro Techniques; D007478:Iontophoresis; D008297:Male; D008875:Middle Aged; D009262:Nails / Q000033:anatomy & histology / Q000187:drug effects* / Q000378:metabolism*; D009281:Naphthalenes / Q000008:administration & dosage* / Q000378:metabolism*; D010539:Permeability / Q000187:drug effects; D011092:Polyethylene Glycols / Q000494:pharmacology*; D000077291:Terbinafine; D014867:Water / Q000378:metabolism
D000277:Adjuvants, Pharmaceutic; D000935:Antifungal Agents; D009281:Naphthalenes; D014867:Water; D011092:Polyethylene Glycols; D000077291:Terbinafine