Interdisciplinary Biotechnology Unit, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, UP, India.
Centre for Biomedical Engineering, Indian Institute of Technology, New Delhi 110016, India.
Int J Pharm. 2024 Oct 25;664:124622. doi: 10.1016/j.ijpharm.2024.124622. Epub 2024 Aug 26.
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 IC 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.
结直肠癌（CRC）是最常见和最具挑战性的恶性肿瘤之一，需要一些有效和更安全的化疗药物进行治疗。在这项研究中，抗癌药物表柔比星（Epi）被负载在聚合物聚乙二醇-聚乳酸-纳米粒子（mPEG-PLA-NPs）中，该纳米粒子由海洋抗癌无毒多糖岩藻聚糖（FC）涂层包裹，以实现对 CRC 的协同作用。对 NPs 的特性进行了研究，结果表明它们是球形的、单分散的、稳定的，具有负的zeta 电位，并具有良好的生物相容性和控制释放。体外研究表明，FC 涂层的 Epi 纳米制剂对 HCT116 细胞系具有良好的抗癌活性，并且与体内研究结果相吻合，体内研究涉及用 C26 鼠癌细胞注射 BALB/C 小鼠。MTT 测定的结果表明，游离 Epi 的 IC 值为 3.72µM，未涂层和涂层的 Epi 纳米制剂的 IC 值分别为 33.67 和 10.19µM。当使用这种新型 NPs 制剂治疗荷瘤小鼠时，观察到更高的肿瘤消退率、更好的存活率和降低的心脏毒性。游离 FC 和 Epi 处理的小鼠的肿瘤大小分别缩小了 37.73%和 61.49%，而未涂层 Epi NPs 和涂层 Epi NPs 处理的小鼠的肿瘤分别缩小了 79.76%和 90.34%。因此，mPEG-PLA-FC-Epi-NPs 有可能被用作有效的治疗 CRC 的化疗制剂，因为它表现出更好的疗效和更低的毒性。
