Bilayered nail lacquer of terbinafine hydrochloride for treatment of onychomycosis.
The present study aimed to develop bilayered nail lacquer of terbinafine hydrochloride (TH) for treatment of onychomycosis. The composite nail lacquer formed an underlying drug-loaded hydrophilic layer and overlying hydrophobic vinyl layer. The hydrophilic lacquer made of hydroxylpropyl methylcellulose E-15 contained polyethylene glycol 400 (PEG 400) as a drug permeation enhancer. The vinyl lacquer was composed of poly (4-vinyl phenol) as a water-resistant film former. In vitro permeation studies in Franz diffusion cells indicated that the amount of TH permeated across the human cadaver nail in 6 days was 0.32 +/- 0.14, 1.12 +/- 0.42, and 1.42 +/- 0.53 microg/cm(2) from control (hydrophilic lacquer devoid of PEG 400), monolayer (hydrophilic lacquer alone), and bilayered nail lacquers, respectively. A higher nail drug load was seen in vitro with the bilayered lacquer (0.59 +/- 0.13 microg/mg) as compared to monolayer (0.36 +/- 0.09 microg/mg) and control (0.28 +/- 0.07 microg/mg) lacquers. The drug loss despite multiple washing was significantly low (p < 0.001) for the bilayered lacquer owing to the protective vinyl coating. Clinical studies demonstrated the efficacy of bilayered lacquer to achieve better drug load in the nail plate (1.27 +/- 0.184 microg/mg) compared to monolayer (0.67 +/- 0.18 microg/mg) and control (0.21 +/- 0.04 microg/mg) lacquers.
Shivakumar
H N
HN
Department of Pharmaceutics, The University of Mississippi, University, Mississippi 38677, USA.
Vaka
Siva Ram Kiran
SR
Madhav
N V Satheesh
NV
Chandra
Harish
H
Murthy
S Narasimha
SN
D000935:Antifungal Agents / Q000008:administration & dosage / Q000032:analysis / Q000627:therapeutic use*; D002102:Cadaver; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D008297:Male; D009262:Nails; D009281:Naphthalenes / Q000008:administration & dosage / Q000032:analysis / Q000627:therapeutic use*; D014009:Onychomycosis / Q000188:drug therapy*; D000077291:Terbinafine
D000935:Antifungal Agents; D009281:Naphthalenes; D000077291:Terbinafine