Arenobufagin（ArBu）是一种天然抗癌药物，具有良好的抗肿瘤效果，但由于其毒性，其临床应用和药物研发潜力受到限制。本研究旨在通过将其纳入聚乙二醇-聚乳酸共聚物（PEG-PLA）中，减少ArBu的毒副作用并提高肿瘤治疗的疗效。通过薄膜水化法制备了ArBu@PEG-PLA微粒。通过大小、稳定性、药物载荷、封装率和药物释放等方面来表征优化后的微粒。在A549细胞和肿瘤小鼠上评价了微粒的抑制肿瘤效果。 ArBu @ PEG-PLA微粒具有良好的药物载荷能力，释放性能和稳定性。它们可以通过EPR效应在肿瘤部位积累。微粒通过线粒体凋亡途径诱导细胞凋亡。与自由ArBu相比，ArBu @ PEG-PLA微粒在急性毒性评估实验中具有更低的毒性和更高的安全性。肿瘤小鼠的体内抗肿瘤实验表明，ArBu@PEG-PLA微粒的肿瘤抑制率为72.9％，比自由ArBu（57.1％）高1.28倍，因此显示出良好的肿瘤治疗效果。本研究表明，ArBu@ PEG-PLA高分子微粒可以显着改善ArBu的毒性和治疗疗效。这些结果可能会导致新的治疗策略，降低ArBu的毒性并增强肿瘤治疗效果。

Arenobufagin (ArBu) is a natural anticancer drug with good anti-tumor effects, but its clinical applications and drug development potential are limited due to its toxicity. The purpose of this study is to reduce the toxic side effects of ArBu and improve the efficacy of tumor treatment by incorporating it into poly(ethylene glycol)-b-poly (lactide) co-polymer (PEG-PLA). ArBu@PEG-PLA micelles were prepared by a thin film hydration method. The optimized micelles were characterized by size, stability, drug loading, encapsulation rate, and drug release. The tumor-inhibition efficacy of the micelles was evaluated on A549 cells and tumor-bearing mice. The ArBu@PEG-PLA micelles have good drug-loading capacity, release performance, and stability. They can accumulate at the tumor site through the EPR effect. The micelles induce apoptosis through a mitochondrial apoptosis pathway. Compared with the free ArBu, the ArBu@PEG-PLA micelles had lower toxicity and higher safety in the acute toxicity evaluation experiment. The in vivo anti-tumor experiment with tumor-bearing mice showed that the tumor-inhibition rate of ArBu@PEG-PLA micelles was 72.9%, which was 1.28-fold higher than that of free ArBu (57.1%), thus showing a good tumor treatment effect. This study indicates that ArBu@PEG-PLA polymeric micelles can significantly improve the toxicity and therapeutic efficacy of ArBu. These can lead to a new therapeutic strategy to reduce the toxicity of ArBu and enhance tumor treatment.