Water-soluble conjugates of protoporphyrin IX (PPix) and cross-linked dextran- coated iron oxide nanoparticles (CLIO NPs) have been designed and synthesized for the delivery of the hydrophobic photosensitizer for photodynamic therapy (PDT) of cancer. The PPix-CLIO NPs conjugates have an average shell-diameter of ca. 77.8 ± 1.6 nm with a magnetite core of ca. 4.03 ± 0.55 nm. When the PPix-CLIO NPs conjugates (0 - 40 μg Fe/mL) were incubated with HeLa cells at 37 ℃ for 12 h, they were taken up, delivering the PPix photosensitizer directly to the intracellular environment. The highly internalizing efficiency of the NPs-conjugates may be attributed to their positive surface potential (12.7 mV) at pH 7.4. Besides, the HeLa cells showed no observable dark toxicity. However, irradiation of the NPs conjugates within the cells by using 312 nm UV-light for 10 min (at co-cultured concentration of 5 μg Fe/mL of PPix-CLIO NPs) causes significant cell mortality through the photodynamic effect. These results suggest that PPix-CLIO NPs conjugates are an excellent vehicle for the delivery of surface-bound hydrophobic photosensitizers for efficient PDT of cultured tumor cells.

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