Microemulsion-loaded hydrogel formulation of butenafine hydrochloride for improved topical delivery

• Published in: Archives of Dermatological Research 2015-09, Vol.307 (7), p.625-633
• Main Authors: Pillai, Anilkumar B., Nair, Jyothilaksmi V., Gupta, Nishant Kumar, Gupta, Swati
• Format: Article
• Language: English
• Subjects: Administration, Topical; Animals; Antifungal Agents - administration & dosage; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; Antifungal Agents - toxicity; Benzylamines - administration & dosage; Benzylamines - chemistry; Benzylamines - pharmacology; Benzylamines - toxicity; Dermatology; Emulsions - chemistry; Hydrogels - chemistry; Hydrogen-Ion Concentration; Medicine; Medicine & Public Health; Naphthalenes - administration & dosage; Naphthalenes - chemistry; Naphthalenes - pharmacology; Naphthalenes - toxicity; Original Paper; Permeability; Rabbits; Skin; Skin Tests; Swine; Toxicity Tests
• ISSN: 0340-3696; 1432-069X
• DOI: 10.1007/s00403-015-1573-z

Topical microemulsion systems for the antifungal drug, butenafine hydrochloride (BTF) were designed and developed to overcome the problems associated with the cutaneous delivery due to poor water solubility. The solubility of BTF in oils, surfactants and co-surfactants was evaluated to screen the components of the microemulsion. Isopropyl palmitate was used as the oil phase, aerosol OT as the surfactant and sorbitan monooleate as co-surfactant. The pseudoternary diagrams were constructed to identify the area of microemulsion existence and optimum systems were designed. The systems were assessed for drug-loading efficiency and characterized for pH, robustness to dilution, globule size, drug content and stability. Viscosity analysis, spreadability, drug content assay, ex vivo skin permeation study and antifungal activity assay were performed for the optimized microemulsion-loaded hydrogel. The optimized BTF microemulsion had a small and uniform globule size. The incorporation of microemulsion system into Carbopol 940 gel was found to be better as compared to sodium alginate or hydroxyl propyl methyl cellulose (HPMC K4 M) gel. The developed gel has shown better ex vivo skin permeation and antifungal activity when compared to marketed BTF cream. Thus, the results provide a basis for the successful delivery of BTF from microemulsion-loaded hydrogel formulation, which resulted in improved penetration of drug and antifungal activity in comparison with commercial formulation of BTF.