PEGYLATED NANOPARTICLES FROM A NOVEL METHOXYPOLYETHYLENE GLYCOL CYANOACRYLATE HEXADECYL CYANOACRYLATE AMPHIPHILIC COPOLYMER

Purpose. The aim of this work was to develop PEGylated poly(alkylcyano acrylate) nanoparticles from a novel methoxypolyethyleneglycol cyanoac rylate-co-hexadecyl cyanoacrylate copolymer. Methods. PEGylated and no n-PEGylated nanoparticles were formed by nanoprecipitation or by emuls ion/solvent evaporation. Nanoparticles size, zeta potential and surfac e hydrophobicity were investigated. Surface chemical composition was d etermined by X-ray photoelectron spectroscopy. Nanoparticle morphology was investigated by transmission electron microscopy after freeze-fra cture. Nanoparticles cytotoxicity was assayed in vitro, onto mouse per itoneal macrophages. Cell viability was determined through cell mitoch ondrial activity, by a tetrazolium-based colorimetric method (MTT test ). Finally, the degradation of PEGylated and non-PEGylated poly(hexade cyl cyanoacrylate) nanoparticles was followed spectrophotometrically d uring incubation of nanoparticles in fetal calf serum. Results. Monodi sperse nanoparticles with a mean diameter ranging between 100 and 200 nm were obtained using nanoprecipitation or emulsion/solvent evaporati on as preparation procedures. A complete physico-chemical characteriza tion, including surface chemical analysis, allowed to confirm the form ation of PEG-coated nanoparticles. The PEGylation of the cyanoacrylate polymer showed reduced cytotoxicity towards mouse peritoneal macropha ges. Furthermore, the presence of the PEG segment increased the degrad ability of the poly(hexadecyl cyanoacrylate) polymer in presence of ca lf serum. Conclusions. We succeeded to prepare PEGylated nanoparticles from a novel poly(methoxypolyethyleneglycol cyanoacrylate-co-hexadecy l cyanoacrylate) by two different techniques. Physico-chemical charact erization showed the formation of a PEG coating layer. Low cytoxicity and enhanced degradation were also shown.