Highly water-soluble and tumor-targeted photosensitizers for photodynamic therapy.

摘要: Biological uses of photosensitizers in photodynamic therapy (PDT) often suffer from a lack tumor selectivity; strategy based on molecule-targeted cancer therapies could provide promising solution. To synthesize new water-soluble phthalocyanines (Pcs) for bio-conjugation with peptides or antibodies, we developed method to asymmetrically substituted Pcs both high water solubility and one monoamino group conjugation biological agents homing, using folic acid as the ligand model direct modified into target cells. Here, report studies syntheses characterization these Pcs. In vitro vivo assays prove that characteristic can greatly increase targeting capability by reducing non-specific uptake. This newly designed photosensitizer accumulated almost completely regions, negligible signal found other tissues xenograft model. These initial data strong evidence specificity folate tri-glycerol substitutions. Theoretically, synthesized be conveniently conjugated many ligands, endorsing broad applicability this tumor-targeted PDT.