title: Microemulsion-based gel of terbinafine for the treatment of onychomycosis: optimization of formulation using D-optimal design.
abstract: The aim of the present investigation was to evaluate microemulsion as a vehicle for dermal drug delivery and to develop microemulsion-based gel of terbinafine for the treatment of onychomycosis. D-optimal mixture experimental design was adopted to optimize the amount of oil (X(1)), Smix (mixture of surfactant and cosurfactant; X(2)) and water (X(3)) in the microemulsion. The formulations were assessed for globule size (in nanometers; Y(1)) and solubility of drug in microemulsion (in milligrams per milliliter; Y(2)). The microemulsion containing 5.75% oil, 53.75% surfactant-cosurfactant mixture and 40.5% water was selected as the optimized batch. The globule size and solubility of the optimized batch were 18.14 nm and 43.71 mg/ml, respectively. Transmission electron microscopy showed that globules were spherical in shape. Drug containing microemulsion was converted into gel employing 0.75% w/w carbopol 934P. The optimized gel showed better penetration and retention in the human cadaver skin as compared to the commercial cream. The cumulative amount of terbinafine permeated after 12 h was 244.65 ± 18.43 μg cm(-2) which was three times more than the selected commercial cream. Terbinafine microemulsion in the gel form showed better activity against Candida albicans and Trichophyton rubrum than the commercial cream. It was concluded that drug-loaded gel could be a promising formulation for effective treatment of onychomycosis.
authors.affiliation: Department of Pharmaceutics, K. B. Institute of Pharmaceutical Education and Research, Kadi Sarva Vishwavidyalaya, Gandhinagar, India. bhaveshbarot83@gmail.com
authors.forename: Bhavesh S
authors.initials: BS
authors.lastname: Barot
authors.forename: Punit B
authors.initials: PB
authors.lastname: Parejiya
authors.forename: Hetal K
authors.initials: HK
authors.lastname: Patel
authors.forename: Mukesh C
authors.initials: MC
authors.lastname: Gohel
authors.forename: Pragna K
authors.initials: PK
authors.lastname: Shelat
mesh_terms: D002176:Candida albicans / Q000187:drug effects / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004655:Emulsions; D005079:Excipients / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D005782:Gels; D009281:Naphthalenes / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D014009:Onychomycosis / Q000188:drug therapy / Q000378:metabolism; D000077291:Terbinafine; D016896:Treatment Outcome; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use
chemical_list: D004655:Emulsions; D005079:Excipients; D005782:Gels; D009281:Naphthalenes; D014344:Trypanocidal Agents; D000077291:Terbinafine