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HPMA 共聚物作为表面活性剂在用于生物医学应用的生物相容纳米粒子的制备中的应用。

HPMA copolymers as surfactants in the preparation of biocompatible nanoparticles for biomedical application.

机构信息

Institute of Organic Chemistry, Johannes Gutenberg-University Mainz, Duesbergweg 10-14, 55128 Mainz, Germany.

出版信息

Biomacromolecules. 2012 Dec 10;13(12):4179-87. doi: 10.1021/bm301453g. Epub 2012 Nov 26.

Abstract

In this work we describe the application of amphiphilic N-(2-hydroxypropyl)methacrylamide (HPMA)-based copolymers as polymeric surfactants in miniemulsion techniques. HPMA-based copolymers with different ratios of HPMA (hydrophilic) to laurylmethacrylate (LMA; hydrophobic) units were synthesized by RAFT polymerization and postpolymerization modification. The amphiphilic polymers can act as detergents in both the miniemulsion polymerization of styrene and the miniemulsion process in combination with solvent evaporation, which was applied to polystyrene and polylactide. Under optimized conditions, monodisperse colloids can be prepared. The most promising results could be obtained by using the block copolymer with a ratio of 90/10. Preliminary cell uptake studies showed that polymer-stabilized nanoparticles have only minor unspecific cellular internalization in HeLa cells. Furthermore, cytotoxicity assays showed no particle-attributed toxicity. In addition, the copolymer-stabilized particles preserved the shape and size in human blood serum as demonstrated by dynamic light scattering.

摘要

在这项工作中,我们描述了两亲性 N-(2-羟丙基)甲基丙烯酰胺 (HPMA) 基共聚物在 miniemulsion 技术中的应用。通过 RAFT 聚合和聚合后修饰合成了具有不同 HPMA(亲水)与月桂基甲基丙烯酸酯(LMA;疏水)单元比例的 HPMA 基共聚物。两亲聚合物可以在苯乙烯的 miniemulsion 聚合和溶剂蒸发相结合的 miniemulsion 工艺中充当表面活性剂,该工艺应用于聚苯乙烯和聚乳酸。在优化条件下,可以制备单分散胶体。使用比例为 90/10 的嵌段共聚物可以获得最有前景的结果。初步的细胞摄取研究表明,聚合物稳定的纳米颗粒在 HeLa 细胞中仅有轻微的非特异性细胞内摄取。此外,细胞毒性测定表明没有颗粒引起的毒性。此外,通过动态光散射证明,共聚物稳定的颗粒在人血清中保持形状和尺寸。

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