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载替莫唑胺的 PLGA 基超顺磁性纳米颗粒用于恶性脑胶质瘤的磁共振成像和治疗。

Temozolomide loaded PLGA-based superparamagnetic nanoparticles for magnetic resonance imaging and treatment of malignant glioma.

机构信息

School of Materials Science and Engineering, South China University of Technology, Guangzhou, Guangdong 510640, China.

出版信息

Int J Pharm. 2012 Jul 1;430(1-2):266-75. doi: 10.1016/j.ijpharm.2012.03.047. Epub 2012 Mar 31.

Abstract

Polysorbate 80 coated temozolomide-loaded PLGA-based superparamagnetic nanoparticles (P80-TMZ/SPIO-NPs) were successfully synthesized and characterized as drug carriers and diagnosis agent for malignant brain glioma. The mean size of P80-TMZ/SPIO-NPs was 220 nm with narrow hydrodynamic particle size distribution. The superparamagnetic characteristic of P80-TMZ/SPIO-NPs was proved by vibration simple magnetometer. P80-TMZ/SPIO-NPs exhibited high drug loading and encapsulation efficiency as well as good sustained drug release performance for 15 days. MTT assay demonstrated the antiproliferative effect of P80-TMZ/SPIO-NPs for C6 glioma cells. Significant cellular uptake of P80-TMZ/SPIO-NPs was evaluated in C6 glioma cells by fluorescence microscopy, Prussian blue staining, and atomic absorption spectrophotometer (AAS) for qualitative and quantitative study, respectively. MRI scanning analyses in vitro indicated that P80-TMZ/SPIO-NPs could be used as a good MRI contrast agent. Polysorbate 80 coated temozolomide-loaded PLGA-based superparamagnetic nanoparticles could be able to promise a multifunctional theragnostic carrier of brain cancer.

摘要

聚山梨酯 80 包裹的替莫唑胺负载的 PLGA 基超顺磁性纳米粒子(P80-TMZ/SPIO-NPs)被成功合成并表征为恶性脑胶质瘤的药物载体和诊断剂。P80-TMZ/SPIO-NPs 的平均粒径为 220nm,具有较窄的水动力粒径分布。振动简谐磁强计证明了 P80-TMZ/SPIO-NPs 的超顺磁性。P80-TMZ/SPIO-NPs 表现出高载药量和包封效率以及良好的持续 15 天的药物释放性能。MTT 测定表明 P80-TMZ/SPIO-NPs 对 C6 神经胶质瘤细胞具有抗增殖作用。通过荧光显微镜、普鲁士蓝染色和原子吸收分光光度计(AAS)分别进行定性和定量研究,评估了 P80-TMZ/SPIO-NPs 在 C6 神经胶质瘤细胞中的摄取情况。体外 MRI 扫描分析表明,P80-TMZ/SPIO-NPs 可用作良好的 MRI 对比剂。聚山梨酯 80 包裹的替莫唑胺负载的 PLGA 基超顺磁性纳米粒子有望成为脑癌的多功能治疗诊断载体。

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