Fouzia GHERRAK
University of Blida, Algeria
Title: Development of a liposomal suspension to increase the skin penetration of Diclofenac
Biography
Biography: Fouzia GHERRAK
Abstract
Several formulation strategies for modifying the skin permeability and for potentiating the activity of an active compound can be envisaged. Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug widely prescribed to treat mild and moderate pain, inflammation and osteoarthritis by inhibiting the enzyme cyclooxygenase. It is already marketed in various forms (gel, emulgel, ophthalmic solution, immediate and prolonged release tablet, suppositories and intramuscular injection). Because of its low solubility in water and in the acidic environment of the stomach, Diclofenac has a low availability and short half-life of about two hours. A topical application for the treatment of rheumatic diseases is therefore suggested to increase bioavailability and decrease toxicity. The objective of this work was to develop a liposomal suspension encapsulating a non-steroidal anti-inflammatory which will constitute the dispersed phase of a gel for dermic use. Diclofenac preparations for dermal application are only marketed in the form gel and emulgel. This liposomal form has been proposed in order to increase the skin penetration or even the availability of Diclofenac thanks to the phospholipidic bilayer of the liposome having the same Structure so that the skin can cross the skin barrier (horny layer). The liposomes were prepared from soy lecithin, cholesterol by the reverse- phase evaporation method. Then analyzed by electron scanning microscope, high-performance liquid chromatography, laser particle size and Zeta-metry to determine their size, encapsulation rate and zeta potential. An optimum with a maximum amount of ethanol in relation to water combined with maximum levels of cholesterol and lecithin was obtained, which promotes the production of small-sized liposomes containing a relatively high surface charge (zeta potential) and having only a narrow polydispersity, thus meeting the stability criteria favoring transposition on an industrial scale.