Nanoemulsion Formulation of Lefl unomide for Transdermal Delivery: Preparation and Characterization

Abstract

Lefl unomide (LEF) is an antirheumatic drug belonging to a class of drugs known as disease modifying antirheumatic drugs, indicated for moderate to severe psoriatic arthritis and rheumatoid arthritis. Orally administrated LEF causes many side eff ects that could result in treatment failure. Hence, in this study, lefl unomide was formulated as a nanoemulsion to develop a transdermal dosage form that can circumvent such side eff ects and increase the rate of successful treatment by improving patient compliance with the medication. The nanoemulsion area was constructed by using pseudo-ternary phase diagrams. A total of 20 nanoemulsion formulas were prepared. These formulas’ mean particle size, zeta potential, and droplet morphology were studied. Thermodynamic stability studies were performed to test the stability of the prepared formulations. Also, the in-vitro release of the drug from the formulations was evaluated using phosphate buff er saline pH 7.4 as the release medium. According to the saturation solubility study results, capryol TM 90 was selected as oil, labrasol and Tween 20 as surfactants for formulation coded A1 and A2, respectively, and transcutol p as cosurfactant together with deionized water as the aqueous phase for the preparation of nanoemulsions. The LEF-nanoemulsion formulations were in the nanosize range (from 54.7–210.2 nm). Images for the chosen formulas revealed dark spherical nanoemulsion droplets against bright surroundings. All of the preparation showed a complete drug release by the end of 220 minutes and the release was highly dependent on the particle size. Based on the result of this study, the prepared LEF-nanoemulsion is successfully prepared and can be considered a promising approach to developing a transdermal preparation.