(232e) Nanoemulsions As Drug Delivery Systems for Poorly Water-Soluble Drugs: Formulation, Transport of Praziquantel Across Caco-2 Cell Monolayers and Cytotoxicity

Nanoemulsions (NEs) are oil-in-water (o/w) dispersions with droplets in the 20–200 nm range. Lipid based formulations have shown their utility to enhance the absorption of poorly absorbable drugs. Praziquantel (PZQ) is a schistosomicidal agent, which is only administrated via the oral route.  High dosages of the drug are used to ensure efficacy to overcome its low bioavailability due to low aqueous solubility.  NEs represent a powerful alternative carrier system to enhance the bioavailability of PZQ because of their high solubilization capacity.

In this presentation we will discuss the compatibility of the NEs with the Caco-2 cell monolayers.  We investigated the cytotoxicity of the NE and the effects of the chemistry of the NE (surfactant, oil phase) in the integrity of polarized Caco-2 monolayers.   Evaluation of the NEs in enhancing intestinal transport will be also discussed and compared with the free drug and a solid nanoparticle formulations, and correlated with the opening of the tight junctions of polarizedCaco-2 cells.