College of Chemistry, Chemical Engineering and Materials Science, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan 250014, China.
J Mater Chem B. 2019 Feb 21;7(7):1149-1159. doi: 10.1039/c8tb03054e. Epub 2019 Jan 30.
Photodynamic therapy (PDT) and photothermal therapy (PTT) are effective cancer treatments, and photosensitizers play the most important role in the treatment. However, photosensitizers are insufficient for in vivo tumor treatment. Herein, we develop a small molecule fluorophore Cy-HPT as a novel photosensitizer, which possesses the advantages of near-infrared (NIR) emission, high photothermal conversion efficiency and high singlet oxygen generation efficiency. Moreover, a nanoplatform of HSA@Cy-HPT was synthesized by self-assembly of Cy-HPT and human serum albumin (HSA) in aqueous solution. Compared to Cy-HPT, HSA@Cy-HPT possesses more stable spectral properties, enhances the effect of PDT/PTT, and exhibits more satisfactory in vivo metabolism. HSA@Cy-HPT demonstrates outstanding tumor targeting in subcutaneous tumor xenograft models owing to its enhanced permeability and retention in tumor tissue. Furthermore, HSA@Cy-HPT was successfully utilized in tumor xenograft models and tumor tissue growth was clearly inhibited without any regrowth, extending survival rate of the models. Also, no distinct damage of the normal tissue of tumor xenograft models was observed using hematoxylin & eosin staining. This study presents a promising therapeutic agent for the synergetic PDT and PTT cancer treatment.
光动力疗法 (PDT) 和光热疗法 (PTT) 是有效的癌症治疗方法，而光敏剂在治疗中起着最重要的作用。然而，光敏剂在体内肿瘤治疗中是不足的。在此，我们开发了一种小分子荧光团 Cy-HPT 作为一种新型光敏剂，它具有近红外 (NIR) 发射、高光热转换效率和高光氧生成效率的优点。此外，通过 Cy-HPT 和人血清白蛋白 (HSA) 在水溶液中的自组装，合成了 HSA@Cy-HPT 纳米平台。与 Cy-HPT 相比，HSA@Cy-HPT 具有更稳定的光谱特性，增强了 PDT/PTT 的效果，并表现出更令人满意的体内代谢。由于 HSA@Cy-HPT 在肿瘤组织中具有增强的通透性和滞留作用，因此在皮下肿瘤异种移植模型中表现出出色的肿瘤靶向性。此外，HSA@Cy-HPT 成功地用于肿瘤异种移植模型，并且肿瘤组织的生长明显受到抑制，没有任何再生，延长了模型的存活率。此外，通过苏木精和伊红染色观察到，肿瘤异种移植模型的正常组织没有明显损伤。这项研究为协同 PDT 和 PTT 癌症治疗提供了一种有前途的治疗剂。
