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两亲自组装“聚合物药物”:纳米粒子的形态、性质和生物学行为。

Amphiphilic self-assembled "polymeric drugs": morphology, properties, and biological behavior of nanoparticles.

机构信息

Institute of Polymer Science and Technology , CSIC, C/Juan de la Cierva 3, 28006 Madrid, Spain.

出版信息

Biomacromolecules. 2012 Mar 12;13(3):624-35. doi: 10.1021/bm300043f. Epub 2012 Feb 29.

Abstract

This article reports the fabrication and characterization of NPs based on the self-assembling of polymeric drugs with amphiphilic character synthetized from oleyl 2-acetamido-2-deoxy-α-d-glucopyranoside methacrylate and vinyl pyrrolidone (OAGMA-VP). NPs were spherical, with an apparent hydrodynamic diameter between 91 and 226 nm and with zeta potential values that ensure stability. Atomic concentrations of C, O, and N, determined by X-ray photoelectron spectroscopy (XPS) of NPs, compared well with the corresponding theoretical values. High resolution XPS C1s spectra suggest that the carbons bound to heteroatoms or carbonyl groups are preferentially situated on the surface of the NP samples. ToF-SIMS spectra analyzed by principal component analysis (PCA) indicated that ions coming from acetyl and oleyl groups of OAGMA play important roles in the outer structure of NPs. Water contact angle and surface tension values of NPs were characteristic of hydrophilic surfaces, confirming the location of VP sequences on the surface. Cell culture assays showed that copolymeric NPs did not compromise biocompatibility of human fibroblasts according to ISO standard, but they were cytotoxic on a human glioblastoma cell line (A-172).

摘要

本文报道了基于具有两亲性的聚合物药物自组装制备纳米粒子(NPs)的方法,该聚合物药物由油酰基 2-乙酰氨基-2-脱氧-α-d-吡喃葡萄糖甲基丙烯酸酯和乙烯基吡咯烷酮(OAGMA-VP)合成。NPs 呈球形,表观水动力直径在 91nm 至 226nm 之间,具有确保稳定性的 ζ 电位值。通过纳米粒子的 X 射线光电子能谱(XPS)测定的 C、O 和 N 的原子浓度与相应的理论值非常吻合。高分辨率 XPS C1s 谱表明,与杂原子或羰基结合的碳原子优先位于 NP 样品的表面。通过主成分分析(PCA)分析的 ToF-SIMS 谱表明,来自 OAGMA 的乙酰基和油酰基的离子在 NPs 的外层结构中起着重要作用。纳米粒子的水接触角和表面张力值呈现亲水表面的特征,证实了 VP 序列位于表面。细胞培养试验表明,根据 ISO 标准,共聚物 NPs 不影响人成纤维细胞的生物相容性,但对人神经胶质瘤细胞系(A-172)具有细胞毒性。

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