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A13458 Triblock copolymers encapsulated poly (aryl benzyl ether) dendrimer zinc(II) phthalocyanine nanoparticles for enhancement in vitro photodynamic efficacy

Objectives: In order to achieve high selectivity and high photodynamic efficacy for therapy of cancer. Methods: A novel series of nanoparticles formed via an electrostatic interaction between the periphery of negatively charged 1–2 generation aryl benzyl ether dendrimer zinc (II) phthalocyanines and positively charged poly(L-lysin) segment of triblock copolymer, poly(L-lysin)-block-poly(ethylene glycol)-blockpoly(L-lysin), was developed for the use as an effective photosensitizers in photodynamic therapy. Results: The dynamic light scattering, atomic force microscopy showed that two nanoparticles has a relevant size of 80–150 nm. The photophysical properties and singlet oxygen quantum yields of free dendrimer phthalocyanines and nanoparticles exhibited generation dependence. The intracellular uptake of dendrimer phthalocyanines in Hela cells was significantly elevated as they were incorporated into the micelles, but was inversely correlated with the generation of dendrimer phthalocyanines. The photocytotoxicity of dendrimer phthalocyanines incorporated into polymeric micelles was also increased. The presence of nanoparticles induced efficient cell death. Using a mitochondrial-sepcific dye rhodamine 123 (Rh123), our fluorescence microscopic result indicated that nanoparticles localized to the mitochondria. Conclusion: G2-DPcZn would be an ideal photosensitizer, and triblock compolymer may be a good carrier for photodynamic therapy of cancer.