Pegylated nanoparticles from a novel methoxypolyethylene glycol cyanoacrylate-hexadecyl cyanoacrylate amphiphilic copolymer.
OBJECTIVE
The aim of this work was to develop PEGylated poly(alkylcyanoacrylate) nanoparticles from a novel methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate copolymer.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Peracchia
M T
MT
Université Paris-Sud XI-URA CNRS 1218, Physico-Chimie-Pharmacotechnie-Biopharmacie, Châtenay-Malabry, France.
Vauthier
C
C
Desmaële
D
D
Gulik
A
A
Dedieu
J C
JC
Demoy
M
M
d'Angelo
J
J
Couvreur
P
P
D000818:Animals; D002460:Cell Line; D003487:Cyanoacrylates; D004337:Drug Carriers; D017737:Macrophages, Peritoneal / Q000187:drug effects*; D051379:Mice; D008854:Microscopy, Electron; D010316:Particle Size; D011092:Polyethylene Glycols; D013052:Spectrometry, X-Ray Emission; D013499:Surface Properties
D003487:Cyanoacrylates; D004337:Drug Carriers; D011092:Polyethylene Glycols