Self-assembled metallocages are very promising drug-delivery systems among supramolecular complexes. Thus, exo-functionalized Pd2 L4 (L=ligand) cages were synthesized and characterized, and the encapsulation of the anticancer drug cisplatin in their cavity has been documented. The antiproliferative effects of the metallocages and their combination with cisplatin were examined in vitro in cancer cell lines, while fluorescence microscopy was used to monitor their uptake. Notably, the hydroxymethyl-functionalized Pd(II) cage encapsulating cisplatin showed improved cytotoxic effect against human ovarian cancer cells compared to free cisplatin. The toxicity of Pd2 L4 cages was evaluated for the first time ex vivo in healthy rat-liver tissues using the precision cut-tissue slices technology, demonstrating in some cases scarce effects on liver viability. These results further highlight the potential of self-assembled Pd2 L4 cages for biological applications.