该研究的主要目的是制备聚合物纳米粒子（NPs）递送5-氟尿嘧啶（FU）的药物递送系统，该系统可以经静脉注射，提高FU的治疗指数。为了实现这一目的，采用界面沉积法制备FU包埋的聚乳酸-聚甘醇酸酯纳米粒子（FU-PLGA-NPs）。评估了不同实验设置对FU整合到NPs的有效性的影响。结果显示，制备有机相的技术和有机相与水相的比率对药物整合到NPs的有效性影响最大。结果显示，制备过程产生了球形、均匀、带负电荷的颗粒，纳米尺寸为200nm，适合静脉注射。药物释放呈双相模式，首先在24小时内快速释放，然后缓慢稳定释放。通过NCI-H69人类小细胞肺癌细胞系评估了FU-PLGA-NPs的体外抗癌潜力。然后与市场上的Fluracil®制剂的体外抗癌潜力进行了比较。还进行了有关Cremophor-EL（Cre-EL）在活细胞上的潜在活性的调查。当NCI-H69细胞暴露于50µg•mL-1 Fluracil®时，其存活率显著降低。研究结果表明，将FU整合到NPs中显著增加了药物对比Fluracil®的细胞毒性效应，这种潜在效应对于较长的孵育时间尤为重要。版权所有©2023 Reem M. Gahtani等。

The major goal of this investigation was to prepare a drug delivery of polymeric nanoparticles (NPs) from 5-fluorouracil (FU) that could be delivered intravenously and improve the therapeutic index of the FU. In order to achieve this, interfacial deposition method was used to prepare FU entrapped poly-(lactic-co-glycolic acid) nanoparticles (FU-PLGA-NPs). The influence of various experimental settings on the effectiveness of FU integration into the NPs was assessed. Our findings show that the technique used to prepare the organic phase and the ratio of the organic phase to the aqueous phase had the greatest impact on the effectiveness of FU integration into NPs. The results show that the preparation process produced spherical, homogenous, negatively charged particles with a nanometric size of 200 nm that are acceptable for intravenous delivery. A quick initial release over 24 h and then slow and steady release of FU from the formed NPs, exhibiting a biphasic pattern. Through the human small cell lung cancer cell line (NCI-H69), the in vitro anti-cancer potential of the FU-PLGA-NPs was evaluated. It was then associated to the in vitro anti-cancer potential of the marketed formulation Fluracil®. Investigations were also conducted into Cremophor-EL (Cre-EL) potential activity on live cells. The viability of NCI-H69 cells was drastically reduced when they were exposed to 50 µg·mL-1 Fluracil®. Our findings show that the integration of FU in NPs significantly increases the drug cytotoxic effect in comparison to Fluracil®, with this potential effect being particularly important for extended incubation durations.Copyright © 2023 Reem M. Gahtani et al.