Nanotechnology is providing a new therapeutic paradigm by enhancing drug efficacy and preventing sideeffects.
Edelfosine is a synthetic ether lipid analogue of platelet activating factor with high antitumor activity. The encapsulation
of this potent antitumor drug in lipid nanoparticles increases its oral bioavailability; moreover, it prevents the
hemolytic and gastrointestinal side-effects of the free drug. The literature points towards lymphatic absorption of lipid
nanoparticles after oral administration, and previous in vitro and in vivo studies stress the protection against toxicity that
these nanosystems provide. The present study is intended to assess the permeability of lipid nanoparticles across the intestinal
barrier. Caco-2 monoculture and Caco-2/Raji co-culture were used as in vitro models of enterocytes and Microfold
cells respectively. Results showed that free drug is internalized and possibly metabolized in enterocytes. These results do
not correlate with those observed in vivo when edelfosine-lipid nanoparticles were administered orally in mice, which
suggests that the microfold model is not a good model to study the absorption of edelfosine-lipid nanoparticles across the
intestinal barrier in vitro.
Keywords: Caco-2, edelfosine, lipid nanoparticles, permeabiltity, raji, transport.
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