title: Formulation development and optimization of transungual drug delivery system of terbinafine hydrochloride for the treatment of onychomycosis.
abstract: The aim of present investigation was to develop transungual drug delivery system (nail lacquer) of terbinafine hydrochloride for treatment of onychomycosis. Different types of penetration enhancers, viz. 2-mercaptoethanol, n-acetyl-L-cysteine and thioglycolic acid, were evaluated to determine their effect on drug permeation. Various types of polymers, both hydrophobic (Eudragit® RL 100 and Eudragit® RS 100) and hydrophilic polymers (hydroxypropyl methyl cellulose (HPMC) E15), were evaluated for their film-forming and drug permeation characteristics. The nail lacquer was optimised statistically by applying 3(2) full factorial design. Polymer ratio (Eudragit® RL 100/HPMC E15; X 1) and solvent ratio (ethanol/water; X 2) were selected as independent variable, and viscosity (cPs), nail plate hydration (%) and in vitro drug permeated at the end of 24 h (μg/cm(2)) were selected as dependent variable. The optimised batch comprises of polymer ratio (70:30) and solvent ratio (75:25). Ex vivo drug permeation study was performed using human cadaver toe nail plate. The results revealed that the amount of drug permeated at the end of 24 h was 61.55 ± 3.2 μg/cm(2), which was found to be higher than the minimum inhibitory concentration of drug. This study confirms that the developed drug-loaded nail lacquer could be used as a promising tool for the effective treatment of onychomycosis.
authors.affiliation: Department of Pharmaceutics, Institute of Pharmacy, Nirma University, SG Highway, Chharodi, Ahmedabad, 382481, Gujarat, India. drmayurmpatel@gmail.com.
authors.forename: Mayur M
authors.initials: MM
authors.lastname: Patel
authors.affiliation: Department of Pharmaceutics, Institute of Pharmacy, Nirma University, SG Highway, Chharodi, Ahmedabad, 382481, Gujarat, India.
authors.forename: Zeal M
authors.initials: ZM
authors.lastname: Vora
mesh_terms: D000111:Acetylcysteine / Q000737:chemistry; D000287:Administration, Topical; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D008623:Mercaptoethanol / Q000737:chemistry; D009262:Nails / Q000378:metabolism*; D009281:Naphthalenes / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D010539:Permeability; D011108:Polymers / Q000737:chemistry; D000077291:Terbinafine; D013864:Thioglycolates / Q000737:chemistry; D014783:Viscosity
chemical_list: D009281:Naphthalenes; D011108:Polymers; D013864:Thioglycolates; D008623:Mercaptoethanol; C017487:2-mercaptoacetate; D000077291:Terbinafine; D000111:Acetylcysteine
keywords: Bovine hoof membranes; Drug permeation; Ex vivo antifungal activity; Nail lacquer; Onychomycosis