Preparation and physicochemical evaluation of transdermal aerosols containing ketoprofen

Abstract

Purpose: To prepare transdermal ketoprofen metered-dose aerosol formulations containing menthol and isopropyl myristate (IPM) as penetration enhancers and to evaluate their physicochemical and permeation properties. Methods: Selected ratios of ketoprofen, ethanol, polyvinylpyrrolidone K30 (PVP K30, anti-nucleant), and penetration enhancers were mixed and filled into aluminum aerosol cans with hydrofluoroalkane-134a as propellant. The physicochemical properties of the films, and their ex vivo permeation properties in rat skin were investigated over a 24-h period. Rat skin was exposed to a definite dose of each ketoprofen film to determine the quantity of drug in the receptor compartment over a 24-h period. Results: All the transdermal formulations showed good integrity and film uniformity. Formulations with permeation enhancers presented higher rates of skin penetration compared to control formulations. Formulations containing 3% PVP and 5% IPM produced the highest permeation rates (Jss, 85.35 µg/cm2/h). Conclusion: These results indicate that incorporation of antinucleant polymer and permeation enhancers in aerosols containing ketoprofen enhances aerosol stability and drug permeation through rat skin.