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Aim: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in cancer treatment. To change the antiviral indication of LAM to anticancer. Background: 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 potential 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. The EE% was at a range of 61–79%. NPs showed prolonged release. The release kinetics were fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have a potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have a 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.

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