Pegylated nanoparticles from a novel methoxypolyethylene glycol cyanoacrylate-hexadecyl cyanoacrylate amphiphilic copolymer

• Published in: Pharmaceutical research Vol. 15; no. 4; pp. 550 - 556
• Main Authors: PERACCHIA, M. T, VAUTHIER, C, DESMAËLE, D, GULIK, A, DEDIEU, J.-C, DEMOY, M, D'ANGELO, J, COUVREUR, P
• Format: Journal Article
• Language: English
• Published: New York, NY Springer 01.04.1998; Springer Nature B.V
• Subjects: Analytical chemistry; Animals; Biological and medical sciences; Cell Line; Copolymers; Cyanoacrylates; Cytotoxicity; Drug Carriers; General pharmacology; Macrophages, Peritoneal - drug effects; Medical sciences; Mice; Microscopy, Electron; Nanoparticles; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polyethylene glycol; Polyethylene Glycols; Polymerization; Polymers; Solvents; Spectrometry, X-Ray Emission; Surface Properties; Biodegradation; Encapsulation; Particle size; Stability; Pharmaceutical technology; Control release polymer; Rodentia; Solubility; Cytotoxicity; Drug carrier; Hydrophobicity; Ethylene oxide polymer; Vertebrata; Mammalia; Mouse; Alkyl acrylate(cyano) polymer; Animal; Established cell line; Dosage form; Acrylate(cyano) copolymer; Surface potential; Physicochemical properties; Macrophage
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1023/A:1011973625803

The aim of this work was to develop PEGylated poly(alkylcyanoacrylate) nanoparticles from a novel methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate copolymer. PEGylated and non-PEGylated nanoparticles were formed by nanoprecipitation or by emulsion/solvent evaporation. Nanoparticles size, zeta potential and surface hydrophobicity were investigated. Surface chemical composition was determined by X-ray photoelectron spectroscopy. Nanoparticle morphology was investigated by transmission electron microscopy after freeze-fracture. Nanoparticles cytotoxicity was assayed in vitro, onto mouse peritoneal macrophages. Cell viability was determined through cell mitochondrial activity, by a tetrazolium-based colorimetric method (MTT test). Finally, the degradation of PEGylated and non-PEGylated poly(hexadecyl cyanoacrylate) nanoparticles was followed spectrophotometrically during incubation of nanoparticles in fetal calf serum. Monodisperse nanoparticles with a mean diameter ranging between 100 and 200 nm were obtained using nanoprecipitation or emulsion/solvent evaporation as preparation procedures. A complete physico-chemical characterization, including surface chemical analysis, allowed to confirm the formation of PEG-coated nanoparticles. The PEGylation of the cyanoacrylate polymer showed reduced cytotoxicity towards mouse peritoneal macrophages. Furthermore, the presence of the PEG segment increased the degradability of the poly(hexadecyl cyanoacrylate) polymer in presence of calf serum. We succeeded to prepare PEGylated nanoparticles from a novel poly(methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate) by two different techniques. Physico-chemical characterization showed the formation of a PEG coating layer. Low cytotoxicity and enhanced degradation were also shown.