Effective Renal Clearance and Photothermal Therapy of a Cyclodextrin-Modified Quaterrylene Derivative

Metabolic clearance of drugs from the body is element for future clinical applications. Compared with the liverbile metabolic route, the renal-urinaryroute is the most desirable and efficient clearance pathway for practical use in clinical trials and can effectively decrease the long-term risk of unpredictable intracellular catabolism and the potential toxicity to normal organs. However, renal clearable photothermal therapy (PTT) agents were limited. In this paper, a permethyl-beta-cyclodextrin-modified quateriylene bisiinide derivative (QDI-CD) was developed. QDI-CD as a biocompatible molecule could effectively be cleared with he renal clearance efficiency of (67.00 +/- 2.37)% at 24 h by the nal-urinary route when administered by tail vein injection. Importantly, the structuref QDI-CD in urine after metabolism does not change. Furthermore, QDI-CD, as a potent photoacoustic and photothermal agent, could effectivly be enriched in tumor tissue after 4 h of injection and showed the effective PTT in mice. This work developed a potent organic PTT agent with good renal clearance from the body and with promise for future clinical applications.