Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer.

Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage.

Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity.

Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined.

Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line.

Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

目的：制备可用于肺癌治疗的拉米夫定（LAM）负载纳米颗粒（NPs）。将LAM的抗病毒适应症改为抗癌。

背景：抗癌药物的开发是一个艰难的过程。加快药物供应的一种方法是将批准用于其他疾病的药物重新归类为抗癌药物。抗癌药物最常见的给药途径是静脉注射。口服抗癌药物可能会大大改变目前化疗的治疗方式，提高癌症患者的生活质量。还有一个潜在的显着经济优势。

目的：表征负载 LAM 的 NPs 并检查抗癌活性。

方法：使用纳米喷雾干燥器制备负载 LAM 的纳米颗粒。通过粒径 (PS)、多分散指数 (PDI)、zeta 电位 (ZP)、SEM、包封效率 (EE%)、溶解、释放动力学、DSC 和 FT-IR 阐明了 NPs 的特性。然后，检查了所有 NPs 的抗癌活性。

结果：加载 LAM 的 NPs 的 PS 值介于 373 和 486 nm 之间。制备的所有纳米颗粒都具有球形结构和正 ZP。EE% 在 61-79% 的范围内。NPs 显示出延长释放和符合威布尔模型的释放动力学。通过 DSC 和 FT-IR 分析阐明了 NPs 结构。结果表明，NPs 的性质与进料溶液的药物：聚合物比直接相关。NPs 在低浓度下对 A549 细胞系具有潜在的抗癌特性，对 CCD 19-Lu 细胞系无毒。

结论：NPs对人肺腺癌细胞具有潜在的抗癌特性，可有效诱导细胞死亡，是治疗此类癌症的有效方式。这些实验还表明我们的制剂对正常细胞无毒。很明显，这项研究将为癌症治疗带来新的视角。