Hydroxycamptothecin (HCPT) is a topoisomerase I inhibitor, and it has been widely used clinically in the treatment of primary liver cancer, gastric cancer, and other tumors. The clinical application of HCPT is limited by its water solubility, and it has certain toxicity to patients with tumor. Therefore, the effective tumor site accumulation of HCPT is necessary. This work studied the inhibitory effect of HCPT on the proliferation and migration of human liver cancer cells (HepG-2) and used carboxymethyl chitosan (CMC) and hyaluronic acid (HA) to modify graphene oxide (GO) as nano-carrier materials, which load HCPT to achieve a drug delivery system for liver tumors with good biocompatibility and high drug loading. HCPT can significantly inhibit proliferation and migration of HepG-2, enhance the release of reactive oxygen species, reduce mitochondrial membrane potential, and induce apoptosis. The GO-CMC-HA/HCPT drug delivery system enabled HepG-2 to uptake more HCPT, thereby inhibiting its proliferation and improving the efficacy of HCPT in vivo and in vitro. This study explored a potential therapy strategy by preparing a GO-based tumor-targeted drug delivery system.

羟基喜树碱（HCPT）是一种拓扑异构酶I抑制剂，临床上广泛用于原发性肝癌、胃癌等肿瘤的治疗。HCPT的临床应用因其水溶性而受到限制，且对肿瘤患者具有一定的毒性。因此，HCPT在肿瘤部位的有效积累是必要的。该工作研究了HCPT对人肝癌细胞（HepG-2）增殖和迁移的抑制作用，并采用羧甲基壳聚糖（CMC）和透明质酸（HA）修饰氧化石墨烯（GO）作为纳米载体材料，负载HCPT，实现具有良好生物相容性和高载药量的肝脏肿瘤药物递送系统。HCPT可显着抑制HepG-2的增殖和迁移，增强活性氧的释放，降低线粒体膜电位，诱导细胞凋亡。GO-CMC-HA/HCPT给药系统使HepG-2能够摄取更多的HCPT，从而抑制其增殖，提高HCPT体内外的疗效。本研究通过制备基于GO的肿瘤靶向药物递送系统来探索潜在的治疗策略。