The aim of this work was the synthesis of a new family of lactosylated piperazinly porphyrins in which the galactoside piperazine moieties are linked to the tetra- and monophenyl ring by an amide bond. Two compounds were designed, synthesized, and characterized by 1H-nuclear magnetic resonance (1H-NMR), ultraviolet (UV)-visible, and matrix-assisted laser desorption/ionization (MALDI) mass spectra. The biological activity on cancer cells and the pharmacokinetics have also been evaluated, showing a very high liver-to-skin ratio and short retentio...