聚乙二醇化聚氰酯毫微粒作为salvicine载体：合成、制备和体外特性

目的：合成和鉴定聚乙二醇化聚氰酯共聚物，制备聚乙二醇化聚氰酯共聚物和聚氰酯聚合物的毫微粒，测定二种毫微粒的体外特性。方法：用^1H-NMR,^13C-NMR和FTIR测定聚乙二醇化聚氰酯共聚物的结构，用凝胶渗透色谱法测定共聚物的分子量，用乳化／蒸发法制备毫微粒。结果：^1H-NMR,^13C-NMR和FTIR光谱与聚乙二醇化聚氰酯共聚物的结构相符，合成共聚物的分子量是6680，用HPLC测定毫微粒的包封效率时，共聚物对salvicine的测定无干扰，聚乙二醇化聚氰酯共聚物毫微粒的包封率是92．6％，聚氰酯聚合物的包封效率是98．9％。二种毫微粒的粒径均为250nm左右。Zeta电位值受聚合物结构的影响，与聚氰酯毫微粒比较（－23．1mV)，聚乙二醇化聚氰酯毫微粒显示低的Zeta电位值（－9.6mV)。毫微粒的体外释放显示一个开始的突释效应，然后缓慢释放达28天。结论：聚乙二醇化聚氰酯毫微粒可能是salvicine体内抗肿瘤作用的一个有效载体。

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

AIM: 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. CONCLUSION: Theseresults showed that the PEGylated PHDCA nanoparticles could be an effective carrier for salvicine delivery in the respect of anti-tumor potency.