This study focuses on the development of a novel liposome-based nanodelivery system designed to encapsulate polyamine-1, a compound with potential anti-tumor properties. The main objective of this work was to enhance the therapeutic and imaging potential of polyamine-1 by incorporating it into liposome-based nanoparticles, which were functionalized with a gadolinium complex for imaging purposes and a fluorescent phospholipid for tracking applications. These nanoparticles were characterized by measuring their size, shape, polydispersity index, zeta potential and encapsulation efficiency. In vitro experiments were conducted to evaluate the antitumor activity, specifically determining the cytotoxicity of both free and encapsulated polyamine-1 in cancerous and non-cancerous cell lines. Additionally, the study shows the enhanced signal intensity of gadolinium-loaded liposomes by T1-weighted MRI, highlighting their imaging potential. The experimental results suggest that this liposome-based nanodelivery system not only has therapeutic potential in targeted cancer therapy but also could be advantageous for diagnostic imaging, particularly in MRI applications.