聚氧乙烯-聚氧丙烯-聚氧乙烯（Poloxamer 188）是一种广泛应用于药物辅料的物质，可以在各种药物制剂中找到。本研究开发了一种新型的自组装纳米平台，用于主动靶向高表达叶酸受体的三阴性乳腺癌。该平台被命名为FPP NPs，由改造过的Poloxamer 188衍生物制备而成，得到了合适尺寸（<100 nm）、良好稳定性和令人满意的生物相容性的纳米颗粒。细胞摄取和体内分布研究表明，FPP NPs在肿瘤细胞摄取和主动靶向方面具有强大的能力。此外，本研究将紫杉醇（DTX）加载到FPP NPs中，所得到的DTX/FPP NPs具有高载药效率和载药量能力，并能在微酸条件下迅速释放DTX，显著增强了体外和体内封装药物的抗肿瘤活性。此外，DTX/FPP NPs还能显著降低DTX的肝毒性和肾毒性。因此，在水溶液中具有自组装特性和向肿瘤主动靶向的改造后的Poloxamer 188基药物传递纳米平台，可能为三阴性乳腺癌的靶向治疗提供了一种有希望的方法。版权所有 © 2023. Elsevier B.V. 发布

Poloxamer 188 is a widely used pharmaceutical excipient, which can be found in a variety of drug formulations. In this study, a novel self-assembled nanoplatform was developed for active targeting of folate receptor-overexpressing triple-negative breast cancer. This platform, FPP NPs, was prepared by the retrofitted poloxamer 188 derivatives, resulting in nanoparticles with an appropriate size (<100 nm), good stability, and satisfactory biocompatibility. Cellular uptake and in vivo distribution studies showed that the FPP NPs had strong tumor cell uptake and active targeting capabilities. Furthermore, docetaxel (DTX) was loaded into FPP NPs in this research. The resulting DTX/FPP NPs exhibited high drug encapsulation efficiency and drug loading capacity, and could rapidly release DTX under slightly acidic conditions, significantly increasing the antitumor activity of the encapsulated drug both in vitro and in vivo. In addition, DTX/FPP NPs could significantly decrease the hepatotoxicity and nephrotoxicity of DTX. Therefore, this drug delivery nanoplatform, based on retrofitted poloxamer 188 with self-assembly properties in aqueous solution and active targeting capabilities to tumors, may provide a promising approach for targeted treatment of triple-negative breast cancer.Copyright © 2023. Published by Elsevier B.V.