PEGylated polycyanoacrylate nanoparticles as salvicine carriers: synthesis, preparation, and in vitro characterization.
OBJECTIVE
To synthesized poly(methoxypolyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate) (PEGylated PHDCA) with polyethylene glycol (PEG, Mr = 5000), prepare PEGylated PHDCA and poly(n-hexadecyl cyanoacrylate) (PHDCA) nanoparticles loading salvicine and determine their in vitro characterizations.


METHODS
The structure of PEGylated PHDCA was determined with 1H-NMR, 13C-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 average molecular weight is 6680. Entrapment efficiency could be determined by high pressure liquid chromatography (HPLC) method without endogenous interference at the retention time of salvicine. The entrapment efficiency was 92.6 % for PEGylated PHDCA nanoparticles and 98.9 % for PHDCA nanoparticles. The nanoparticles size was about 250 nm. The values of the zeta potential were 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.


CONCLUSIONS
These results showed that the PEGylated PHDCA nanoparticles could be an effective carrier for salvicine delivery in the respect of anti-tumor potency.
Li
Y P
YP
Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China. ypli@mail.shcnc.ac.cn
Zhou
Z H
ZH
Pei
Y Y
YY
Zhang
X Y
XY
Gu
Z H
ZH
Yuan
W F
WF
D003487:Cyanoacrylates / Q000138:chemical synthesis* / Q000737:chemistry; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D036103:Nanotechnology; D009285:Naphthoquinones / Q000032:analysis* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry
D003487:Cyanoacrylates; D004337:Drug Carriers; D009285:Naphthoquinones; C121140:polyethyleneglycol polyhexadecylylcyanoacrylate copolymer; C122096:salvicine; D011092:Polyethylene Glycols