植物来源的黄酮类化合物槲皮素（Q）具有广泛的抗癌潜力和相应的分子机制，在体外的细胞模型中已有大量的文献资料。然而，由于槲皮素的低生物利用度和亲水性，其在生物医学应用中的限制很大。本研究采用电纺技术制备了基于聚乳酸（PLA）和聚乙烯氧化物（PEO）的Q载药微纳纤维，分别为PLA/Q和PLA/PEO/Q非织造布的形式。通过扫描电子显微镜和原子力显微镜（SEM和AFM）、X射线粉末衍射（XRD）、差示扫描量热（DSC）、接触角测量、傅立叶变换红外光谱（FTIR）和拉曼光谱对载药纤维的结构和物化性质进行了表征。利用两种癌细胞和九个细胞系，即骨肉瘤（MG-63，U-2 OS，SaOS-2细胞）和乳腺癌（SK-BR-3，MCF-7，MDA-MB-231，MDA-MB-468，Hs 578T和BT-20细胞）揭示了PLA/Q和PLA/PEO/Q的抗癌作用。载药纤维的抗癌活性比游离的槲皮素更显著。PLA/Q和PLA/PEO/Q促进了细胞周期阻滞、氧化应激和凋亡细胞死亡，这种效应不能被热休克蛋白（HSP）介导的适应性反应所克服。通过体外测试使用正常成纤维细胞评判，证实PLA/Q和PLA/PEO/Q具有生物相容性和安全性。我们推测，具有释放槲皮素活性的PLA/Q和PLA/PEO/Q可被视为一种新颖且更高效的微纳系统，用于释放槲皮素并消除表型不同的癌细胞。 版权所有 © 2023 作者。由Elsevier B.V.出版。保留所有权利。

The anticancer potential of quercetin (Q), a plant-derived flavonoid, and underlining molecular mechanisms are widely documented in cellular models in vitro. However, biomedical applications of Q are limited due to its low bioavailability and hydrophilicity. In the present study, the electrospinning approach was used to obtain polylactide (PLA) and PLA and polyethylene oxide (PEO)-based micro- and nanofibers containing Q, namely PLA/Q and PLA/PEO/Q, respectively, in a form of non-woven fabrics. The structure and physico-chemical properties of Q-loaded fibers were characterized by scanning electron and atomic force microscopy (SEM and AFM), X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), goniometry and FTIR and Raman spectroscopy. The anticancer action of PLA/Q and PLA/PEO/Q was revealed using two types of cancer and nine cell lines, namely osteosarcoma (MG-63, U-2 OS, SaOS-2 cells) and breast cancer (SK-BR-3, MCF-7, MDA-MB-231, MDA-MB-468, Hs 578T, and BT-20 cells). The anticancer activity of Q-loaded fibers was more pronounced than the action of free Q. PLA/Q and PLA/PEO/Q promoted cell cycle arrest, oxidative stress and apoptotic cell death that was not overcome by heat shock protein (HSP)-mediated adaptive response. PLA/Q and PLA/PEO/Q were biocompatible and safe, as judged by in vitro testing using normal fibroblasts. We postulate that PLA/Q and PLA/PEO/Q with Q releasing activity can be considered as a novel and more efficient micro- and nano-system to deliver Q and eliminate phenotypically different cancer cells.Copyright © 2023 The Authors. Published by Elsevier B.V. All rights reserved.