β-Cyclodextrine-based polyester was coated on the surface of gadolinium oxide nanoparticles (NPs) and then functionalised with folic acid to produce an efficient pH-sensitive targeted theranostic system (Gd2O3@PCD-FA) for doxorubicin delivery and magnetic resonance imaging (MRI). Gd2O3@PCD-FA was fully characterised by FTIR, vibrating sample magnetometer, TGA, XRD, SEM and TEM analyses. The dissolution profile of DOX showed a pH sensitive release. No significant toxicity was observed for the targeted NPs (Gd2O3@PCD-FA) and DOX-loaded NPs inhibiting M109 cells viability more efficiently than free DOX. Moreover, the negligible hemolytic activity of the targeted NPs showed their appropriate hemocompatibility. The preferential uptake was observed for the developed Gd2O3@PCD-FA-DOX NPs in comparison with Dotarem using T1- and T2-weighted MRI in the presence of folate receptor-positive and folate receptor-negative cancer cells (M109 and 4T1, respectively). Furthermore, in vivo studies revealed that Gd2O3@PCD-FA-DOX not only exhibited considerably relaxivity performance as a contrast agent for MRI, but also improved in vivo anti-tumour efficacy of the system. The results suggest that Gd2O3@PCD-FA-DOX improves its therapeutic efficacy in the treatment of solid tumours and also reduces the adverse effects, so it could be proposed as a promising drug delivery system for chemotherapy and molecular imaging diagnosis in MRI.

中文翻译：

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载有阿霉素的环糊精基聚酯改性氧化钆纳米颗粒的体外和体内特性：用于肿瘤化疗和分子共振成像的多功能靶向治疗系统。

β-环糊精基聚酯涂覆在氧化钆纳米颗粒 (NPs) 的表面，然后用叶酸功能化以产生有效的 pH 敏感靶向治疗系统 (Gd2O3@PCD-FA)，用于多柔比星递送和磁共振成像 (MRI) ）。Gd2O3@PCD-FA 通过 FTIR、振动样品磁强计、TGA、XRD、SEM 和 TEM 分析进行了全面表征。DOX 的溶出曲线显示出 pH 敏感的释放。没有观察到靶向 NPs (Gd2O3@PCD-FA) 和 DOX 负载的 NPs 比游离 DOX 更有效地抑制 M109 细胞活力的显着毒性。此外，靶向 NPs 的溶血活性可忽略不计，表明它们具有适当的血液相容性。在叶酸受体阳性和叶酸受体阴性癌细胞（分别为 M109 和 4T1）存在的情况下，使用 T1 和 T2 加权 MRI 观察到开发的 Gd2O3@PCD-FA-DOX NPs 与 Dotarem 相比优先摄取. 此外，体内研究表明，Gd2O3@PCD-FA-DOX 作为 MRI 造影剂不仅表现出显着的弛豫性能，而且还提高了系统的体内抗肿瘤功效。结果表明，Gd2O3@PCD-FA-DOX提高了其在实体瘤治疗中的疗效，并减少了不良反应，因此可作为一种有前景的药物递送系统用于化疗和MRI分子成像诊断。体内研究表明，Gd2O3@PCD-FA-DOX 作为 MRI 造影剂不仅表现出显着的弛豫性能，而且还提高了该系统的体内抗肿瘤功效。结果表明，Gd2O3@PCD-FA-DOX提高了其在实体瘤治疗中的疗效，并减少了不良反应，因此可作为一种有前景的药物递送系统用于化疗和MRI分子成像诊断。体内研究表明，Gd2O3@PCD-FA-DOX 作为 MRI 造影剂不仅表现出显着的弛豫性能，而且还提高了该系统的体内抗肿瘤功效。结果表明，Gd2O3@PCD-FA-DOX提高了其在实体瘤治疗中的疗效，并减少了不良反应，因此可作为一种有前景的药物递送系统用于化疗和MRI分子成像诊断。