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Self-assembled polyion complex micelles for sustained release of hydrophilic drug

机译:自组装的聚离子复合物胶束,用于持续释放亲水性药物

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Graft copolymer polyethylenimine-graft-poly(A/-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.
机译:使用N,N'-二环己基碳二亚胺(DCC)和N-羟基琥珀酰亚胺通过单羧基封端的PVP(PVP-COOH)与PEI偶联制备接枝共聚物聚乙烯亚胺-接枝-聚(A /-乙烯基吡咯烷酮)(PEI-g-PVP) (NHS)作为偶联剂。在水性介质中,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)一起自组装成稳定的聚离子复合胶束( PVP-b-PAMPS)。透射电子显微镜图像显示这些胶束呈规则球形。通过尺寸分析确定的胶束尺寸为约142nm。为了评估其作为药物媒介物的可行性,将模型药物叶酸(FA)通过静电相互作用掺入胶束的核心。 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胶束具有作为药物输送纳米载体的巨大潜力。

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