Institute of Fine Chemical and Engineering, Henan University, Kaifeng, Henan 475001, China.
J Microencapsul. 2011;28(2):93-8. doi: 10.3109/02652048.2010.534823.
Graft copolymer polyethylenimine-graft-poly(N-vinylpyrrolidone) (PEI-g-PVP) was prepared by coupling mono carboxyl-terminated PVP (PVP-COOH) with PEI using N,N'-dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (NHS) as coupling agents. In aqueous medium, PVP-g-PEI can self-assemble into stable polyion complex micelles with an oppositely charged block copolymer, poly(N-vinylpyrrolidone)-block-poly(2-acrylamido-2-methyl-1-propanesulphonic acid) (PVP-b-PAMPS). Transmission electron microscopy images showed that these micelles were regularly spherical in shape. The micelle size determined by size analysis was around 142 nm. To estimate their feasibility as vehicles for drugs, the model drug folic acid (FA) was incorporated into the cores of the micelles via electrostatic interactions. In vitro release test of FA showed that the drug-release rates are dependent on the pH value of the release media. Based on these results, we can conclude that the polyion complex micelles prepared from the PEI-g-PVP/PVP-b-PAMPS copolymers have great potential as drug delivery nanocarriers.
接枝共聚物聚乙烯亚胺接枝聚（N-乙烯基吡咯烷酮）（PEI-g-PVP）是通过使用 N，N'-二环己基碳二亚胺（DCC）和 N-羟基琥珀酰亚胺（NHS）作为偶联剂将单羧基封端的 PVP（PVP-COOH）与 PEI 偶联制备的。在水介质中，PVP-g-PEI 可以与带相反电荷的嵌段共聚物聚（N-乙烯基吡咯烷酮）-嵌段-聚（2-丙烯酰胺基-2-甲基-1-丙磺酸）（PVP-b-PAMPS）自组装成稳定的聚离子复合物胶束。透射电子显微镜图像显示，这些胶束呈规则的球形。通过粒径分析确定的胶束粒径约为 142nm。为了评估它们作为药物载体的可行性，通过静电相互作用将模型药物叶酸（FA）掺入胶束的核中。FA 的体外释放试验表明，药物释放速率取决于释放介质的 pH 值。基于这些结果，我们可以得出结论，由 PEI-g-PVP/PVP-b-PAMPS 共聚物制备的聚离子复合物胶束作为药物传递纳米载体具有很大的潜力。
