Kidney Disease Center, The First Affiliated Hospital, Zhejiang University School of Medicine, Key Laboratory of Kidney Disease Prevention and Control Technology, National Key Clinical Department of Kidney Diseases, Institute of Nephrology, Zhejiang University, Hangzhou, Zhejiang Province 310003, China.
Zhejiang Clinical Research Center of Kidney and Urinary System Disease, Hangzhou, Zhejiang Province 310003, China.
Nano Lett. 2023 Jun 28;23(12):5641-5647. doi: 10.1021/acs.nanolett.3c01235. Epub 2023 Jun 9.
Acute kidney injury (AKI) is a common clinical syndrome lacking effective pharmacotherapy. Gambogic acid (GA), as an active ingredient of herbal medicines, exhibits antioxidant and anti-inflammatory effects that benefit the treatment of AKI, but its poor aqueous solubility limits effective renal delivery. We, for the first time, developed GA-based nanoparticles (GA-NPs) with preferential renal uptake for AKI treatment. By PEGylating with NH-PEG5000-NOTA, hydrophobic GA was self-assembled into ∼4.5 nm nanoparticles, which showed the enhanced renal accumulation in AKI models from PET images. Importantly, the cell assays and tests of the two AKI models have confirmed the obvious nephroprotective effects and biosafety of GA-NPs. Therefore, this work indicates that GA-NPs can be a promising therapeutic candidate for the management of AKI.
急性肾损伤（AKI）是一种常见的临床综合征，缺乏有效的药物治疗。藤黄酸（GA）作为一种草药的有效成分，具有抗氧化和抗炎作用，有利于 AKI 的治疗，但它的低水溶性限制了其在肾脏中的有效传递。我们首次开发了基于 GA 的纳米颗粒（GA-NPs），用于 AKI 的治疗，具有优先的肾脏摄取。通过 NH-PEG5000-NOTA 的聚乙二醇化，疏水性 GA 自组装成约 4.5nm 的纳米颗粒，在 AKI 模型的 PET 图像中显示出增强的肾脏积累。重要的是，两种 AKI 模型的细胞测定和试验证实了 GA-NPs 的明显的肾脏保护作用和生物安全性。因此，这项工作表明 GA-NPs 可能是一种有前途的治疗 AKI 的候选药物。
