In vitro evaluation of a novel amphotericin B-loaded nanoemulsion: chemical stability and antifungal activity

F.B. Filippin-Monteiro, I.F. Kretzer, R.C. Maranhão, L.C. Souza
Federal University of Santa Catarina, BR

Keywords: amphotericin B, nanostructured lipid carriers, antifungal activity, ultrasonic irradiation

Summary:

In an attempt to overcome the solubility issues of AB using excipients that are already in use for parenteral administration, we proposed a novel nanoemulsion system with high volume fraction of oil phase including combinations of medium and long chain triglycerides and nonionic surfactants designed to achieve a drug delivery systems in aqueous media. Formulations were prepared by ultrasonic method using combinations of medium chain triglycerides (MCT) (Miglyol 812N®) or long chain triglycerides (LCT) (oleic acid glyceride) and soy (SL) or egg lecithin (EL), following by 30 or 45-minute sonication. Nanoemulsions presented narrow droplet size ranging from 100 to 150 nm (Figure 1D) and the MCT/SL combination was chosen. Since physicochemical properties were suitable for stable nanoparticles, cytotoxicity and antifungal activity were performed. Cytotoxicity against kidney cells of AB-containing formulations was similar to non-containing one. In addition, AB-Ns presented interesting activity against Candida albicans isolates suggesting antifungal properties with low toxicity towards kidney cells. The physicochemical data obtained in the present study suggest that this nanoemulsion system shows an attractive potential as drug delivery system. Advantages of this technique are ease of manufacturing, use of biocompatible components for parenteral administration, and production in aqueous media avoiding organic solvents.