Pitavastatin-containing nanoemulsions: Preparation, characterization and in vitro cytotoxicity

The aim of this study was to prepare pitavastatin-containing nanoemulsions in order to increase intestinal absorption. The effects of the charges of the nanoemulsions and of other physicochemical key properties were studied. The nanoemulsions were produced with a microfluidization method using different homogenization pressures, durations and temperatures. The nanoemulsions were characterized by measuring the droplet size, size distribution, zeta potential and permeability as well as cytotoxicity using Caco-2 cells. Five hundred bar, 15 °C and 3 min were needed for producing positively charged nanoemulsions (droplet size: 306 nm, polydispersity index: 0.36; zeta potential: 35 mV), while 4 min were needed for preparing negatively charged nanoemulsions (droplet size: 179 nm, polydispersity index: 0.15, zeta potential: −45 mV). The cytotoxicity studies using Caco-2 cells revealed that both types of nanoemulsions, positively and negatively charged, were not cytotoxic. The positively charged nanoemulsions showed the highest permeation through Caco-2 cell lines, compared to the negatively charged nanoemulsions and a drug solution. The increased permeation of the positively charged nanoemulsion can serve as a sign for a possible increased bioavailability and can probably enhance the absorption of the drug.

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