To overcome the obstacles inflicted by the BBB in Glioblastoma multiforme (GBM) we investigated the use of Multifunctional nanoparticles that designed with a Nano-graphene oxide (NGO) sheet functionalized with magnetic poly (lactic-co-glycolic acid) (PLGA) and was used for glioma targeting delivery of radiosensitizing 5-iodo-2-deoxyuridine (IUdR). In vitro biocompatibility of nanocomposite has been studied by the MTT assay. In vivo efficacy of magnetic targeting on the amount and selectivity of magnetic nanoparticles accumulation in glioma-bearing rats under an external magnetic field (EMF) density of 0.5 T was easily monitored with MRI. IUdR-loaded magnetic NGO/PLGA with a diameter of 71.8 nm, a zeta potential of −33.07 ± 0.07 mV, and a drug loading content of 3.04 ± 0.46% presented superior superparamagnetic properties with a saturation magnetization (Ms) of 15.98 emu/g. Furthermore, Prussian blue staining showed effective magnetic targeting, leading to remarkably improved tumor inhibitory efficiency of IUdR. The tumor volume of rats after treatment with IUdR/NGO/SPION/PLGA + MF was decreased significantly compared to the rats treated with buffer saline, IUdR and SPION/IUdR/NGO/PLGA. Most importantly, our data demonstrate that IUdR/NGO/SPION/PLGA at the present magnetic field prolongs the median survival time of animals bearing gliomas (38 days, p < 0.01). Nanoparticles also had high thermal sensitivities under the alternating magnetic field. In conclusion, we developed magnetic IUdR/NGO/PLGA, which not only achieved to high accumulation at the targeted tumor site by magnetic targeting but also indicated significantly enhanced therapeutic efficiency and toxicity for glioma both in vitro and in vivo. This innovation increases the possibility of improving clinical efficiency of IUdR as a radiosensitizer, or lowering the total drug dose to decrease systemic toxicity.

为克服BBB在多形胶质母细胞瘤（GBM）中造成的障碍，我们研究了多功能纳米颗粒的使用，该纳米颗粒设计了用磁性聚乳酸-乙醇酸乙醇（PLGA）功能化的纳米氧化石墨烯（NGO）片材，用于靶向放射增敏性5-碘-2-脱氧尿苷（IUdR）的神经胶质瘤。通过MTT分析研究了纳米复合材料的体外生物相容性。磁靶向对体内神经胶质瘤大鼠在0.5 T的外部磁场（EMF）密度为0.5 T时磁性纳米颗粒积累的数量和选择性的体内功效很容易通过MRI进行监测。载有IUdR的磁性NGO / PLGA，直径为71.8 nm，ζ电位为-33.07±0.07 mV，载药量为3.04±0。46％的人具有优异的超顺磁性，饱和磁化强度（Ms）为15.98 emu / g。此外，普鲁士蓝染色显示出有效的磁靶向性，从而显着提高了IUdR的肿瘤抑制效率。与用缓冲盐水，IUdR和SPION / IUdR / NGO / PLGA治疗的大鼠相比，用IUdR / NGO / SPION / PLGA + MF治疗的大鼠的肿瘤体积明显减少。最重要的是，我们的数据表明，在目前的磁场下，IUdR / NGO / SPION / PLGA延长了患有神经胶质瘤的动物的中位生存时间（38天，p <0.01）。纳米粒子在交变磁场下也具有很高的热敏性。总之，我们开发了磁性IUdR / NGO / PLGA，它不仅通过磁性靶向实现了在靶肿瘤部位的高积累，而且还表明了在体外和体内对神经胶质瘤的治疗效率和毒性都大大提高了。这项创新增加了提高IUdR作为放射增敏剂的临床效率或降低总药物剂量以降低全身毒性的可能性。