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硫酸软骨素-g-聚(ε-己内酯)共聚物聚集体作为潜在的靶向药物载体。

Chondroitin sulfate-g-poly(ϵ-caprolactone) co-polymer aggregates as potential targeting drug carriers.

作者信息

Wang Li-Fang, Ni Hsiao-Chen, Lin Chia-Chan

机构信息

a Faculty of Medicinal and Applied Chemistry, School of Life Science, Kaohsiung Medical University , 100 Shih-Chuan 1st Road , Kaohsiung City , 80708 , Taiwan.

出版信息

J Biomater Sci Polym Ed. 2012;23(14):1821-42. doi: 10.1163/156856211X598210. Epub 2012 May 11.

Abstract

The aim of this study is to delineate the effect of various amounts of hydrophobic polycaprolactone (PCL) grafted onto three different degrees of methacrylated chondroitin sulfate (CSMA) on chemical-physical properties. The co-polymers were prepared by reacting the modified PCL and the hydrophilic CSMA via a radical reaction (CSMA-PCL). The effect of degree of methacrylation of CSMA and feed ratio between CSMA and PCL on compositions and critical micelle concentrations was systematically studied. The PCL composition of the CSMA-PCL was characterized by (1)H-NMR and FT-IR. The hydrodynamic diameters and morphologies of CSMA-PCL micelles were studied by DLS and TEM. Critical micelle concentrations were determined using pyrene as a probe. Taking one of the CSMA-PCL micelles as an example, a cancer-mediated ligand, folic acid, was linked to the surface. The cellular uptake of the folic acid-linked CSMA-PCL in folate-receptor-overexpressing KB cells was studied by confocal laser scanning microscopy and flow cytometry.

摘要

本研究的目的是描述接枝到三种不同甲基丙烯酸化程度的硫酸软骨素(CSMA)上的不同量疏水聚己内酯(PCL)对化学物理性质的影响。通过自由基反应使改性PCL与亲水性CSMA反应制备共聚物(CSMA-PCL)。系统研究了CSMA的甲基丙烯酸化程度以及CSMA与PCL之间的进料比对组成和临界胶束浓度的影响。通过(1)H-NMR和FT-IR对CSMA-PCL的PCL组成进行了表征。通过动态光散射(DLS)和透射电子显微镜(TEM)研究了CSMA-PCL胶束的流体力学直径和形态。使用芘作为探针测定临界胶束浓度。以其中一种CSMA-PCL胶束为例,将癌症介导配体叶酸连接到其表面。通过共聚焦激光扫描显微镜和流式细胞术研究了叶酸连接的CSMA-PCL在叶酸受体过表达的KB细胞中的细胞摄取情况。

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