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Preparation and characterization of cationic Pluronic for surface modification and functionalization of polymeric drug delivery nanoparticles

机译:阳离子Pluronic的制备和表征,用于高分子药物递送纳米颗粒的表面改性和功能化

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摘要

Biodegradable poly(lactic-co-glycolic acid) copolymer, PLGA nanoparticles (NPs) with a surface layer of poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymers, Pluronics, are promising drug carrier systems. With the aim to increase the potential of targeted drug delivery the end group derivative of Pluronics was synthesized in a straightforward way to obtain Pluronic-amines. The formation of functional amine groups was confirmed by fluorescamine method and NMR analysis of their Boc-Phe-OH and Fmoc-Phe-OH conjugates. Pluronic and Pluronic-amine stabilized PLGA NPs prepared by nanoprecipitation were characterized by dynamic light scattering and zeta potential measurements. All of the systems showed high colloidal stability checked by electrolyte induced aggregation, although the presence of Pluronic-amine on the surface decreased the zeta potential in some extent. The introduction of reactive primary amine groups into the surface layer of PLGA NPs while preserving the aggregation stability, provides a possibility for coupling of various ligands allowing targeted delivery and also contributes to the improved membrane affinity of NPs.ud
机译:具有聚(环氧乙烷)-聚(环氧丙烷)-聚(环氧乙烷)三嵌段共聚物,Pluronics表面层的可生物降解的聚乳酸-乙醇酸共聚物,PLGA纳米颗粒(NPs)是很有前途的药物载体系统。为了增加靶向药物递送的潜力,以直接的方式合成了Pluronics的端基衍生物以获得Pluronic-胺。通过荧光胺法和其Boc-Phe-OH和Fmoc-Phe-OH共轭物的NMR分析证实了官能胺基团的形成。通过动态光散射和ζ电位测量对通过纳米沉淀法制备的Pluronic和Pluronic胺稳定的PLGA NP进行了表征。尽管表面上存在Pluronic胺,但在一定程度上降低了Zeta电位,所有的系统均表现出了高的胶体稳定性,可通过电解质诱导的聚集进行检查。在保持聚集稳定性的同时,将反应性伯胺基团引入PLGA NP的表面层,为偶联各种配体提供了可能性,从而可以靶向递送,还有助于提高NPs的膜亲和力。

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