Single laser activated photodynamic/photothermal cancer therapy using a single mitochondria-targeted phototherapeutic agent with aggregation-induced emission characteristics

Abstract

Simultaneous photodynamic therapy (PDT) and photothermal therapy (PTT) have aroused a broad range of interest for improving therapeutic efficacy due to the advantage of the synergistic effect. Conventional synergistic PDT/PTT agents are mainly multi-components that need complex preparation processes and multiple irradiation sources. Additionally, subcellular organelle-targeting capability is also very important for improving therapeutic efficacy. However, the development of a single-component mitochondria-targeted agent for synergistic PDT/PTT therapy remains a challenging task. Herein, we synthesized an electron donating–accepting conjugated phototherapeutic agent (OPTM) with aggregation-induced emission (AIE) properties and mitochondria-targeting ability through reasonable molecular design, and constructed multifunctional OPTM nanoparticles (OPTM NPs) by encapsulating OPTM with polymer F127. Notably, OPTM NPs have specific mitochondria-targeting capability, excellent reactive oxygen species generation for PDT, high photothermal conversion efficiency for PTT and photothermal imaging ability. Impressively, OPTM NPs as an efficient mitochondria-targeted agent can be successfully employed for a synergistic phototherapy in vivo under single laser irradiation.