Folic acid is often used for active targeting of tumor cells to enhance therapeutic outcomes. Here, folic acid was conjugated with chitosan and folate-conjugated chitosan-lipid hybrid nanoparticles were prepared by ionic gelation method using anionic lipid. These nanoparticles were in size range of 200 to 400 nm with spherical shape. In vitro drug release data suggested a sustained release of cisplatin. The therapeutic efficacy of the folate-conjugated hybrid nanoparticles was evaluated in SK-OV-3, A2780 and MCF-7 cancer cell lines. A significant increase in cytotoxicity was observed with folate targeted LPHNPs compared to non-targeted LPHNPs. Significantly enhanced cellular uptake and cell cycle arrest resulting from folate-targeted nanoparticles were confirmed using fluorescence microscopy and flow cytometry. The therapeutic efficacy and tumor penetration were further evaluated in 3D spheroid tumor models. These studies suggest that folate-conjugated lipid-chitosan nanoparticles could enhance therapeutic activity and may represent a promising platform for active targeting of tumor cells.

叶酸通常用于主动靶向肿瘤细胞以增强治疗效果。在此，将叶酸与壳聚糖偶联，并使用阴离子脂质通过离子凝胶法制备了与叶酸偶联的壳聚糖-脂质杂化纳米颗粒。这些纳米颗粒具有球形的200至400nm的尺寸范围。体外药物释放数据表明顺铂持续释放。在SK-OV-3，A2780和MCF-7癌细胞系中评估了叶酸偶联杂化纳米颗粒的治疗效果。与非靶向LPHNPs相比，叶酸靶向LPHNPs的细胞毒性显着增加。使用荧光显微镜和流式细胞术证实了叶酸靶向的纳米颗粒显着增强了细胞摄取和细胞周期停滞。在3D球形肿瘤模型中进一步评估了治疗效果和肿瘤穿透力。这些研究表明，叶酸缀合的脂质-壳聚糖纳米颗粒可以增强治疗活性，并且可以代表有希望的平台来主动靶向肿瘤细胞。