Design and evaluation of microemulsion gel system of nadifloxacin

Abstract

Topical microemulsion systems for the antiacne agent, nadifloxacin were designed and developed to overcome the problems associated with the cutaneous delivery due to poor water solubility. The solubility of nadifloxacin in oils, surfactants and cosurfactants was evaluated to screen the components of the microemulsion. Various surfactants and cosurfactants were screened for their ability to emulsify the selected oily phase. The pseudoternary diagrams were constructed to identify the area of microemulsion existence. The influence of km (surfactant/cosurfactant) ratio on the microemulsion existence region was determined and optimum systems were designed. The systems were assessed for drug-loading efficiency and characterised for optical birefringence, pH and refractive index, robustness to dilution, globule size, drug content and thermodynamic stability. Optimised microemulsion systems were formulated into gel form and evaluated for viscosity, spreadability, drug content, ex vivo skin permeation and antibacterial activity. The maximum solubility of nadifloxacin in the microemulsion system was found to be 0.25%. The nadifloxacin microemulsions had a small and uniform globule size (67.3-121.23 nm). The stability results revealed that all formulations showed a stable globule size and the polydispersity index under stress conditions. Incorporation of nadifloxacin in microemulsion gel increased the ex vivo skin permeation and antibacterial activity when compared to marketed cream.