多叶假组织培养双花皂苷D（PD）是一种类固醇皂苷，可通过内在的凋亡途径诱导不同癌症类型的细胞凋亡。然而，新兴证据表明，PD的结构的溶血和细胞毒性是其主要问题。本研究旨在开发和优化PD负载的固体脂质纳米粒（SLN）配方，并评估其在乳腺癌细胞系中的疗效。通过流式细胞术检测Annexin V / propidium iodide染色和Western blot分析，确认了凋亡作为细胞死亡机制。在体内研究中，使用不同剂量的PD负载的SLN对4T1移植BALB / c小鼠的肿瘤抑制效果进行了比较。 PD-负载的SLN的半数抑制浓度（IC50）分别为33.25和35.74μg / mL。流式细胞术分析进一步证实，在PD负载的SLN处理后，细胞凋亡显著增加。当两种细胞系都接受PD负载的SLN处理时，Bcl2和HSP70蛋白被下调，而Bax、Bad、P53、Apaf-1、p-p53和Noxa蛋白被上调。这种效应也通过在BALB / c小鼠体内进行的测试得到证实。基于这些结果，PD负载的SLN可能是一种有前途的乳腺癌治疗方法，没有明显的副作用。版权所有© 2023 Elsevier B.V。

Polyphyllin D (PD), a steroidal saponin in Paris polyphylla, induces apoptosis via the intrinsic apoptotic pathway in different cancer types. However, emerging evidence has shown that the primary issue with PD is its structure's hemolysis and cytotoxicity. This study aimed to develop and optimize PD-loaded SLN formulation and evaluate its efficacy in breast cancer cell lines. Apoptosis, as the mechanism of cell death, was confirmed by flow cytometry following Annexin V/propidium iodide staining and western blot analysis. In in vivo studies, tumor inhibitory efficacy was compared with different doses of PD-loaded SLN on 4T1-implanted BALB/c mice. The half-maximal inhibitory concentration (IC50) of PD- loaded SLN was calculated to be 33.25 and 35.74 μg/mL for MCF7 and MDA-MB-231 cells, respectively. Flow cytometry analysis further confirmed a significant increase in apoptosis after treatment with PD- loaded SLN. When both cell lines were treated with PD-loaded SLN, Bcl2 and HSP70 proteins were down regulated, while Bax, Bad, P53, Apaf-1, p-p53 and Noxa proteins were upregulated. This effect was also confirmed by test performed on BALB/c mice in vivo. Based on results, PD-loaded SLN may be a promising breast cancer treatment, without recognizable side effects.Copyright © 2023 Elsevier B.V. All rights reserved.