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Polymeric nanoparticles could offer promising controlled drug delivery. The biocompatibility is of extreme importance for future applications in humans. Self-assembled polymeric nanoparticles based on phenylalanine ethyl ester (PAE)-modified alginate (Alg) had been successfully prepared and characterized in our lab. However, little is known about their interaction with cells and other biological systems. In this study, nanoparticles (NPs) based on PAE-Alg conjugates (PEA-NPs) with different degree of substitution (DS) were prepared and investigated. Our results showed that PEA-NPs had no effects on the proliferation of the human intestinal epithelial Caco-2 cells at concentrations up to 1000 μg/mL. Furthermore, the in vitro cellular uptake profile of PEA-NPs, concerning several parameters involved in the application of therapeutic or diagnostic NPs, such as NPs concentration, time and temperature, was described. Different NPs have been adopted for cellular uptake studies and the NPs internalized into Caco-2 cells were quantified. Cellular uptake efficiency could reach 60% within 4 h. PEA-NPs also showed greater cell permeability than oleoyl alginate ester nanoparticles (OAE-NPs) previously prepared in our lab. Our studies reveal that NPs based on PEA conjugate are promising nanosystems for cellular delivery.

Biocompatibility Profile and In Vitro Cellular Uptake of Self-assembled Alginate Nanoparticles