title: Investigation of the Dermal Absorption and Irritation Potential of Sertaconazole Nitrate Anhydrous Gel.
abstract: Effective topical therapy of cutaneous fungal diseases requires the delivery of the active agent to the target site in adequate concentrations to produce a pharmacological effect and inhibit the growth of the pathogen. In addition, it is important to determine the concentration of the drug in the skin in order to evaluate the subsequent efficacy and potential toxicity for topical formulations. For this purpose, an anhydrous gel containing sertaconazole nitrate as a model drug was formulated and the amount of the drug in the skin was determined by in vitro tape stripping. The apparent diffusivity and partition coefficients were then calculated by a mathematical model describing the dermal absorption as passive diffusion through a pseudo-homogenous membrane. The skin irritation potential of the formulation was also assessed by using the in vitro Epiderm™ model. An estimation of the dermal absorption parameters allowed us to evaluate drug transport across the stratum corneum following topical application. The estimated concentration for the formulation was found to be higher than the MIC100 at the target site which suggested its potential efficacy for treating fungal infections. The skin irritation test showed the formulation to be non-irritating in nature. Thus, in vitro techniques can be used for laying the groundwork in developing efficient and non-toxic topical products.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA. mahima.manian@live.mercer.edu.
authors.forename: Mahima
authors.initials: M
authors.lastname: Manian
authors.affiliation: Department of Pharmacy Practice, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA. kumpal.madrasi@gmail.com.
authors.forename: Kumpal
authors.initials: K
authors.lastname: Madrasi
authors.affiliation: Department of Pharmacy Practice, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA. ayyappach@gmail.com.|Department of Pharmacotherapy, University of North Texas Health Science Center, Fort Worth, Texas 76107, USA. ayyappach@gmail.com.
authors.forename: Ayyappa
authors.initials: A
authors.lastname: Chaturvedula
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA. banga_ak@mercer.edu.
authors.forename: Ajay K
authors.initials: AK
authors.lastname: Banga
keywords: dermal absorption; diffusion model; sertaconazole nitrate; skin irritation; topical