PEGylated polycyanoacrylate nanoparticles as salvicine carriers: synthesis, preparation, and in vitro characterization

AIM: To synthesized poly( methoxypolyethyleneglycol cyanoacrylate-co-n-hexa decyl cyanoacrylate)( PEGylated PHDCA) with polyethylene glycol (PEG, M-r = 5000), prepare PEGylated PHDCA and poly ( n-hexadecyl cyanoacrylate) (PHDC A) nanoparticles loading salvicine and determine their in vitro characteriz ations. METHODS: The structure of PEGylated PHDCA was determined with H-1-N MR, C-13-NMR and Fourier transform infrared spectrum (FTIR). Its molecular weight was determined by gel permeation chromatography (GPC). Nanoparticles were prepared by emulsion/solvent evaporation method. RESULTS: 1H-NMR, 13C -NMR, and FTIR were consistent with structure of PEGylated PHDCA, whose ave rage molecular weight is 6680. Entrapment efficiency could be determined by high pressure liquid chromatography (HPLC) method without endogenous inter ference at the retention time of salvicine. The entrapment efficiency was 9 2.6 % for PEGylated PHDCA nanoparticles and 98.9 % for PHDCA nanoparticles. The nanoparticles size was about 250nm. The values of the zeta potential w ere obviously influenced by the composition of the copolymer. Compared with PHDCA nanoparticles (-23.1 mV), PEGylated PHDCA nanoparticles showed a low surface potential (- 9.6 mV). Salvicine release from nanoparticles showed an initial burst effect, then a plateau for an extended period, and finally sustained release phase. CONCLUSION: These results showed that the PEGylat ed PHDCA nanoparticles could be an effective carrier for salvicine delivery in the respect of anti-tumor potency.