Microemulsion-based antifungal gel of luliconazole for dermatophyte infections: formulation, characterization and efficacy studies

Abstract

Luliconazole (LZ), a poorly water soluble synthetic imidazole derivative is used in the treatment of fungal infections of skin. Hence, the investigation was aimed at formulating microemulsion based gels (MBGs) for solubilization of LZ as well as its better penetration for efficacious anti-fungal treatment. The solubility of LZ in various oils was investigated. Out of tried oils, olive oil exhibited highest solubility. Suitable combination of surfactants and co-surfactants were screened for selected oil to yield O/W type microemulsion. The Pseudoternary phase diagrams were developed to determine microemulsion existence area. The developed microemulsion was evaluated for particle size analysis, isotropicity, pH, drug content and rheology. Drug loaded microemulsion was slowly added to the viscous solution of 1 % Carbomer 934 under magnetic stirring to prepare MBG. The prepared MBG were evaluated in terms of their droplet size, spreadability, stability, in vitro permeation studies, and rheological properties. The phase study revealed that the maximum proportion of oil was incorporated in microemulsion systems when the surfactant-to-cosurfactant ratio was 3:1. The microemulsion was optimized with its components of Olive oil as oil, Capmul MCM as a surfactant and iso propyl alcohol as a cosurfactant. The globule size of the optimized batch was 32.59 nm. The MBG was non-irritant indicating their safety and was active against C. albicans indicating its efficacy. Short term stability study performed as per ICH guideline exhibited stable characteristic of developed formulation. Therefore, MBG of LZ is an efficacious treatment for fungal infections.