Fan Kexin, Li Qingyang, Qian Yuping, Zhang Ludan, Lu Di, Zhu Ling, Yan Shouke, Xu Bowei, Wang Yuguang
State Key Laboratory of Chemical Resource Engineering, College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, China.
Department of General Dentistry II, Peking University School and Hospital of Stomatology & National Center for Stomatology & National Clinical Research Center for Oral Diseases & National Engineering Research Center of Oral Biomaterials and Digital Medical Devices Beijing Key Laboratory of Digital Stomatology & NHC Key Laboratory of Digital Stomatology & NMPA Key Laboratory for Dental Materials & Central Laboratory, Peking University School and Hospital of Stomatology, Beijing, 100081, PR China.
Adv Healthc Mater. 2025 Jan;14(2):e2403248. doi: 10.1002/adhm.202403248. Epub 2024 Nov 18.
Due to the inadequate photothermal conversion efficiency (PCE), most photothermal agents (PTAs) have to be used under high-power near-infrared (NIR) irradiation, which significantly exceeds medical safety standards, for achieving effective photothermal therapy (PTT) in antitumor treatment. This significantly hinders practical PTT application. Herein, three acceptor-donor-acceptor(A-D-A)-type molecules are synthesized based on cyclopentadithiophene unit to develop effective PTAs. By incorporating the large-size Si atom in the A-D-A molecules, the photosensitizer displays an increased packing distance in the aggregate state, leading to a blue-shifted absorption spectrum that better matches the medial laser wavelength. Also, the Si incorporation strategy elevates the nonradiative decay rate constants (k) of the A-D-A photosensitizer, and thereby a further enhancement in PCE is achieved for the PTA. Consequently, the SiO-4F-based nanoparticles exhibited 64.23% PCE, with excellent biosafety and photothermal stability. Under NIR irradiation with medical safety (808 nm, 0.33 W cm), SiO-4F nanoparticles with 100 µg mL yield a death rate of over 91% for diverse tumor cells. Moreover, in vivo experiments, SiO-4F-based PTT effectively inhibited and eliminated tumors. These findings suggest that the Si-incorporated CDPT is promising for constructing effective A-D-A photosensitizers, enabling the PTT under NIR irradiation that meets medical safety standards.
由于光热转换效率(PCE)不足,大多数光热剂(PTA)在抗肿瘤治疗中为了实现有效的光热疗法(PTT),不得不使用远高于医学安全标准的高功率近红外(NIR)照射。这严重阻碍了PTT的实际应用。在此,基于环戊二噻吩单元合成了三种受体-供体-受体(A-D-A)型分子,以开发有效的PTA。通过在A-D-A分子中引入大尺寸的Si原子,光敏剂在聚集态下表现出增加的堆积距离,导致吸收光谱蓝移,更好地匹配医用激光波长。此外,Si掺入策略提高了A-D-A光敏剂的非辐射衰减速率常数(k),从而使PTA的PCE进一步提高。因此,基于SiO-4F的纳米颗粒表现出64.23%的PCE,具有优异的生物安全性和光热稳定性。在医用安全的近红外(808 nm,0.33 W cm)照射下,浓度为100 μg mL的SiO-4F纳米颗粒对多种肿瘤细胞的死亡率超过91%。此外,在体内实验中,基于SiO-4F的PTT有效地抑制和消除了肿瘤。这些发现表明,掺入Si的CDPT有望构建有效的A-D-A光敏剂,实现符合医学安全标准的近红外照射下的PTT。