The delivery of therapeutic nucleic acids is a prospective method for the treatment of both inherited and acquired diseases including cancer. To achieve maximal delivery efficiency and selectivity, nucleic acids should be targeted to the cells of interest. In the case of cancer, such targeting may be provided through folate receptors overexpressed in many tumor cells. For this purpose, folic acid and its lipoconjugates are used. Compared to other targeting ligands, folic acid provides low immunogenicity, rapid tumor penetration, high affinity to a wide range of tumors, chemical stability, and easy production. Different delivery systems can utilize targeting by folate ligand including liposomal forms of anticancer drugs, viruses, and lipid and polymer nanoparticles. This review focuses on the liposomal gene delivery systems that provide targeted nucleic acid transport into tumor cells due to folate lipoconjugates. Moreover, important development step, such as rational design of lipoconjugates, folic acid content, size, and ζ-potential of lipoplexes are discussed.