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磁性热敏氟尿嘧啶胶束的制备与表征

Preparation and characterization of magnetic thermosensitive fluorouracil micelles.

作者信息

Zhang Min, Jin Xueqin, Gou Guojing

机构信息

a Department of Pharmacy, College of Pharmacy , Ningxia Medical University , Yinchuan.

出版信息

J Biomater Sci Polym Ed. 2016;27(8):773-91. doi: 10.1080/09205063.2016.1162626. Epub 2016 Mar 30.

Abstract

In this study, we synthesized P(NIPAM-co-DMAM)-b-PLA polymers with free radical polymerization and ring-opening addition polymerization, and immediately assembled 'dextran magnetic layered double hydroxide fluorouracil' (DMF) magnetic particles into the core of the amphiphilic polymer micelles with synchronous hydration and dialysis, to generate a magnetic thermosensitive fluorouracil drug delivery system. The basic properties of the micelle particles, such as the core-shell-type structure, size, and zeta potential, were studied with (1)H-NMR, FTIR, TEM, TGA, laser nanoparticle size analysis, and other characterization techniques. The thermosensitivity of the micelles was investigated by measuring parameters such as the lower critical solution temperature (LCST) and the relationship between the particle size variation and temperature. The drug release curves for the micelles at different temperatures were constructed with a dialysis method. The LCST of the triblock polymers was 42 °C. The particle sizes of the blank micelles and DMF-loaded micelles were 493.6 ± 1.8 nm and 464.9 ± 4.1 nm, respectively, at 25 °C. When the temperature was higher than LSCT, a contraction phase change in the micelle structure occurred, a significant characteristic of the core-shell-type structure, and reversible phase transition phenomena. The release behavior of the drug-loaded micelles showed obvious variations with temperature. Therefore, the magnetic thermosensitive fluorouracil drug delivery system has a good magnetic response and excellent temperature controlled release characteristics, so it can be used as a drug delivery system in magnetically and thermally targeted chemotherapy for tumors.

摘要

在本研究中,我们通过自由基聚合和开环加成聚合合成了P(NIPAM-co-DMAM)-b-PLA聚合物,并通过同步水合和透析将“葡聚糖磁性层状双氢氧化物氟尿嘧啶”(DMF)磁性颗粒立即组装到两亲聚合物胶束的核心中,以生成磁性热敏氟尿嘧啶药物递送系统。使用(1)H-NMR、FTIR、TEM、TGA、激光纳米颗粒尺寸分析和其他表征技术研究了胶束颗粒的基本性质,如核壳型结构、尺寸和zeta电位。通过测量诸如最低临界溶液温度(LCST)以及粒径变化与温度之间的关系等参数来研究胶束的热敏性。采用透析法构建了胶束在不同温度下的药物释放曲线。三嵌段聚合物的LCST为42℃。在25℃时,空白胶束和负载DMF的胶束的粒径分别为493.6±1.8nm和464.9±4.1nm。当温度高于LSCT时,胶束结构发生收缩相变,这是核壳型结构的一个显著特征,以及可逆相变现象。载药胶束的释放行为随温度呈现明显变化。因此,磁性热敏氟尿嘧啶药物递送系统具有良好的磁响应和优异的温度控释特性,因此可作为肿瘤磁热靶向化疗中的药物递送系统。

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