State Key Laboratory of Fine Chemicals, Dalian University of Technology, 2 Linggong Road, Hi-Tech Zone, Dalian, 116024, China.
State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, Chinese Academy of Sciences, Beijing, 100190, China.
Adv Mater. 2020 Mar;32(11):e1907855. doi: 10.1002/adma.201907855. Epub 2020 Feb 5.
Traditional photothermal therapy requires high-intensity laser excitation for cancer treatments due to the low photothermal conversion efficiency (PCE) of photothermal agents (PTAs). PTAs with ultra-high PCEs can decrease the required excited light intensity, which allows safe and efficient therapy in deep tissues. In this work, a PTA is synthesized with high PCE of 88.3% based on a BODIPY scaffold, by introducing a CF "barrier-free" rotor on the meso-position (tfm-BDP). In both the ground and excited state, the CF moiety in tfm-BDP has no energy barrier to rotation, allowing it to efficiently dissipate absorbed (NIR) photons as heat. Importantly, the barrier-free rotation of CF can be maintained after encapsulating tfm-BDP into polymeric nanoparticles (NPs). Thus, laser irradiation with safe intensity (0.3 W cm , 808 nm) can lead to complete tumor ablation in tumor-bearing mice after intravenous injection of tfm-BDP NPs. This strategy of "barrier-free rotation" provides a new platform for future design of PTT agents for clinical cancer treatment.
传统的光热疗法由于光热剂（PTAs）的光热转换效率（PCE）低，因此需要高强度激光激发来进行癌症治疗。具有超高 PCE 的 PTAs 可以降低所需的激发光强度，从而允许在深部组织中进行安全有效的治疗。在这项工作中，基于 BODIPY 支架合成了一种 PTA，其 PCE 高达 88.3%，通过在中位（tfm-BDP）上引入 CF“无阻碍”转子。在基态和激发态下，tfm-BDP 中的 CF 部分没有旋转的能量障碍，使其能够有效地将吸收的（近红外）光子转化为热量。重要的是，将 tfm-BDP 封装在聚合物纳米颗粒（NPs）中后，无阻碍旋转的 CF 可以保持。因此，静脉注射 tfm-BDP NPs 后，用安全强度（0.3 W cm, 808nm）的激光照射可以导致荷瘤小鼠的肿瘤完全消融。这种“无阻碍旋转”策略为未来用于临床癌症治疗的 PTT 剂的设计提供了新的平台。
