Ovarian cancer has a poor prognosis due to late diagnosis, frequent recurrence, and limited therapeutic options. Potent topoisomerase I inhibitors exhibit substantially higher cytotoxic potency than conventional chemotherapeutic agents but often suffer from poor aqueous solubility and limited permeability, restricting their direct clinical application. Therefore, the development of an effective delivery platform for these agents is essential to improve their therapeutic potential. In this study, we developed peptide-targeted liposomes (PTL) encapsulating a potent topoisomerase I inhibitor to enhance tumor cell targeting and intracellular drug delivery in ovarian cancer. The liposomes were prepared using a thin-film hydration method and evaluated in comparison with non-targeted liposomes (PL) and the free drug. The peptide-targeted formulation demonstrated improved colloidal stability during storage and sustained drug release behavior relative to the free drug. In ovarian cancer cells, PTL showed enhanced cellular uptake and greater antiproliferative activity compared with PL. Furthermore, in an ovarian tumor xenograft mouse model, PTL achieved significantly greater tumor growth inhibition than both PL and the free drug. Collectively, these findings suggest that peptide-targeted liposomal delivery represents a promising strategy to enhance the therapeutic efficacy of topoisomerase I inhibitors for ovarian cancer treatment.