聚乙二醇化聚氰基丙烯酸酯纳米颗粒作为肿瘤坏死因子-α载体
PEGylated polycyanoacrylate nanoparticles as tumor necrosis factor-alpha carriers.
作者信息
Li Y P, Pei Y Y, Zhou Z H, Zhang X Y, Gu Z H, Ding J, Zhou J J, Gao X J
机构信息
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, China.
出版信息
J Control Release. 2001 Apr 28;71(3):287-96. doi: 10.1016/s0168-3659(01)00235-8.
The aim of this study was to find an effective carrier for recombinant human tumor necrosis factor-alpha (rHuTNF-alpha). The influence of solvent systems containing poly(methoxy-polyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate) (PEGylated PHDCA) on the biological activity of rHuTNF-alpha was investigated. The PEGylated PHDCA nanoparticles loading rHuTNF-alpha were prepared with the double emulsion method. The influence of main experimental factors on the entrapment efficiency was evaluated by the Uniform Design. The physicochemical characteristics and in vitro release of rHuTNF-alpha from the nanoparticles were determined. The results showed that serum albumin such as human serum albumin (HSA) or bovine serum albumin (BSA) could play a protective action on rHuTNF-alpha in the preparation process. At > or =2.0% (w/v) HSA concentration, more than 85% of rHuTNF-alpha activity remained and the role of HSA was not affected by copolymer concentrations from 0.5 to 3.0% (w/v). The entrapment efficiency of the nanoparticles was about 60% and the nanoparticle size was about 150 nm. The nanoparticles were spherical in shape and uniform with the value of the zeta potential about -9 mV. The rHuTNF-alpha release from the nanoparticle showed an initial burst and then continued in a sustained fashion. The results showed that the PEGylated PHDCA nanoparticles could be an effective carrier for rHuTNF-alpha.
本研究的目的是寻找一种重组人肿瘤坏死因子-α（rHuTNF-α）的有效载体。研究了含有聚（甲氧基聚乙二醇氰基丙烯酸酯-co-正十六烷基氰基丙烯酸酯）（聚乙二醇化PHDCA）的溶剂体系对rHuTNF-α生物活性的影响。采用复乳法制备了负载rHuTNF-α的聚乙二醇化PHDCA纳米粒。通过均匀设计评估了主要实验因素对包封率的影响。测定了纳米粒的理化特性以及rHuTNF-α的体外释放情况。结果表明，血清白蛋白如人血清白蛋白（HSA）或牛血清白蛋白（BSA）在制备过程中对rHuTNF-α可起到保护作用。当HSA浓度≥2.0%（w/v）时，超过85%的rHuTNF-α活性得以保留，且HSA的作用不受共聚物浓度从0.5%至3.0%（w/v）的影响。纳米粒的包封率约为60%，粒径约为150 nm。纳米粒呈球形且均匀，zeta电位值约为-9 mV。rHuTNF-α从纳米粒中的释放呈现出初始突释，然后持续释放的特点。结果表明，聚乙二醇化PHDCA纳米粒可能是rHuTNF-α的有效载体。
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