Abstract The aim of this study is to explore the kidney-targeting capability of mesoscale nanoparticles (MNPs)-emodin (Em-MNPs) and its potential antifibrosis in the animal model. First, MNPs and Em-MNPs were synthesized via nanoprecipitation method, and their diameters were both ∼400 nm with the uniform size. The entrapment efficiency of MNPs was 45.1% when adding emodin at the concentration of 12 mg/mL. Moreover, cytotoxicity assay showed that Em-MNPs presented excellent biocompatibility in rat proximal tubular cells. Cellular uptake assay demonstrated that Em-MNPs had high-efficiency uptake, especially in the cytoplasm. Ex vivo organ fluorescence imaging revealed that Em-MNPs possessed specific kidney-targeting ability with relative long retention time in the kidney (∼24 h). In the renal unilateral ureteral obstruction model, Em-MNPs treatment could significantly alleviate kidney tubule injury and reduce extracellular matrix deposition compared with free MNPs. Herein, Em-MNPs with specific kidney-targeting and preferable antifibrosis effects in animal model may pave an avenue for treating renal diseases.

中文翻译：

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用大黄素封装的中尺度纳米粒子用于靶向动物模型中的抗纤维化

摘要 本研究的目的是探索中尺度纳米颗粒 (MNPs)-大黄素 (Em-MNPs) 的肾脏靶向能力及其在动物模型中的潜在抗纤维化作用。首先，通过纳米沉淀法合成了 MNPs 和 Em-MNPs，它们的直径都在 400 nm 左右，尺寸均匀。当添加浓度为 12 mg/mL 的大黄素时，MNPs 的包封率为 45.1%。此外，细胞毒性试验表明，Em-MNPs 在大鼠近端肾小管细胞中表现出优异的生物相容性。细胞摄取试验表明，Em-MNPs 具有高效摄取，尤其是在细胞质中。离体器官荧光成像显示，Em-MNPs 具有特定的肾脏靶向能力，在肾脏中的保留时间相对较长（~24 小时）。在肾单侧输尿管梗阻模型中，与游离 MNPs 相比，Em-MNPs 治疗可以显着减轻肾小管损伤并减少细胞外基质沉积。在此，在动物模型中具有特异性肾脏靶向和较好抗纤维化作用的 Em-MNPs 可能为治疗肾脏疾病铺平道路。