The conjugation of targeted therapy and image-guided phototdynamic therapy of cancer in vitro and in vivo.

Abstract Integration of multi-functional diagnosis and treatment competencies can improve effect of the drug and its visual distribution to the location of tumor focus site, and play a pivotal role by visualizing the tumor size in the assessment of chemotherapy. With the objective of developing integrated multi-therapeutic and diagnostic agent that could target the kinase receptor with high expression in tumor cells, herein, a biologically releasable drug-drug conjugate compound 9 with dual therapeutic and diagnostic effects was designed, synthesized and evaluated for pharmacodynamics and diagnostic functions in vitro and in vivo. The results of antitumor effects evaluations and compound 9 visual imaging indicated that compound 9 not only improved the anti-proliferative activity of chemotherapy and photodynamic treatment (PDT) in vitro and in vivo compared with those of compound 8 and PpIX but also allowed the photodynamic diagnosis (PDD). The present study verified a facile and effective strategy using a drug-drug conjugate to integrate diagnosis and multi-therapies, showing its potential a candidate clinical drug.