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Drugs with positive charge usually have good water solubility, enhanced cellular uptake efficiency and activity. However, the preparation of quaternized drugs need potentially dangerous agents, while protonated cationic drugs are easily deprotonated in alkaline solutions. Arginine can be positively charged in a wide range of pH. Thus, two phthalocyanine-arginine conjugates (ArgEZnPc and ArgZnPc) were reported in this paper. They can be positively charged in the range of pH 5 to 9. Besides, the photochemical and photobiological properties, subcellular localization, anticancer activities of the them were also carried out. The results show that ArgEZnPc has high water solubility, excellent singlet oxygen and reactive oxygen species generation efficiency, can preferentially localize in the lysosomes of HeLa cells.