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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,~(13)C-NMR和FTIR测定聚乙二醇化聚氨酯共聚物的结构,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,~(13)C-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。
OBJECTIVE: To synthesize and identify PEGylated poly (cyanoethylene glycol) copolymer, prepare nanoparticles of PEGylated poly (cyanoacrylate) copolymer and poly (cyanoacrylate) polymer, and determine in vitro properties of the two nanoparticles. METHODS: The structures of PEGylated polyurethane copolymers were determined by ~ 1H-NMR, ~ (13) C-NMR and FTIR. The molecular weights of the copolymers were determined by gel permeation chromatography. The nanoparticles were prepared by emulsification / evaporation. Results: The 1H-NMR, ~ (13) C-NMR and FTIR spectra were consistent with the structure of PEGylated poly (cyanoethylene glycol) copolymer. The molecular weight of the synthesized copolymer was 6680. When the encapsulation efficiency of nanoparticles was measured by HPLC, The copolymer did not interfere with the determination of salvicine, and the encapsulation efficiency of the PEGylated poly (ethylene glycol) copolymer nanoparticles was 92.6%. The encapsulation efficiency of the polyurethane polymer was 98.9%. Two kinds of nanoparticles are about 250nm particle size. Zeta potential values were influenced by the polymer structure, as compared to the poly (cyano) nanoparticles (-23.1 mV) and the PEGylated nanoparticles showed a low Zeta potential (-9.6 mV). In vitro release of nanoparticles showed an initial burst effect and then slowly released for 28 days. CONCLUSION: Pegylated polycyanocaproic nanoparticles may be an effective carrier of anti-tumor effect of salvicine in vivo.