结直肠癌（CRC）是最常见和最具挑战性的恶性肿瘤之一，需要一些有效且更安全的化疗药物进行治疗。在这项研究中，抗癌剂表柔比星（Epi）被负载在涂有海洋抗癌无毒多糖岩藻依聚糖（FC）的聚合聚乙二醇-聚乳酸纳米粒子（mPEG-PLA-NPs）中，以实现对抗癌的协同活性。 CRC。纳米颗粒的表征表明它们呈球形、单分散、稳定、具有负zeta电位，并表现出良好的生物相容性和控释性。 NPs 对 HCT116 细胞系的体外抗癌活性被发现是有前景的，并且与注射 C26 鼠癌细胞的 BALB/C 小鼠的体内研究得到了很好的证实。 MTT测定结果表明，游离Epi纳米制剂的IC50值为3.72 µM，未包衣和包衣Epi纳米制剂的IC50值分别为33.67和10.19 µM。当这种新型纳米颗粒制剂用于治疗荷瘤小鼠时，观察到更高的肿瘤消退、更好的存活率和降低的异常心脏毒性。游离 FC 和 Epi 治疗的小鼠的肿瘤大小分别缩小了 37.73% 和 61.49%，而用未包被的 Epi NP 和包被的 Epi NP 处理的小鼠的肿瘤大小分别为 79.76% 和 90.34%。因此，mPEG-PLA-FC-Epi-NPs 有潜力用作针对 CRC 的有效化疗制剂，因为它表现出更好的疗效和更低的毒性。版权所有 © 2024 Elsevier B.V. 保留所有权利。

Colorectal cancer (CRC) is one of the most common and challenging malignancy that needs some effective and safer chemotherapeutic agents for the treatment. In this study, anticancer agent epirubicin (Epi) was loaded in polymeric polyethylene glycol-polylactic acid-nanoparticles (mPEG-PLA-NPs) coated with a marine anti-cancer non-toxic polysaccharide fucoidan (FC), to achieve a synergistic activity against CRC. The characterization of the NPs revealed that they were spherical, monodispersed, stable, with a negative zeta potential, and exhibited good biocompatibility and controlled release. In vitro anti-cancer activity of the NPs on HCT116 cell line was found to be promising, and corroborated well with in vivo studies involving BALB/C mice injected with C26 murine cancer cells. The outcome of MTT assay demonstrated that IC50 value of free Epi was 3.72 µM, and that of non-coated and coated Epi nano-formulations was 33.67 and 10.19 µM, respectively. Higher tumor regression, better survival and reduced off-side cardiotoxicity were observed when this novel NPs formulation was used to treat tumor-bearing mice. Free FC and Epi treated mice showed 37.73 % and 61.49 % regression in tumor size, whereas there was 79.76 % and 90.34 % tumor regression in mice treated with non-coated Epi NPs and coated Epi NPs, respectively. Therefore, mPEG-PLA-FC-Epi-NPs hold a potential to be used as an effective chemotherapeutic formulation against CRC, since it exhibited better efficacy and lower toxicity.Copyright © 2024 Elsevier B.V. All rights reserved.