CAS Key Laboratory of Soft Matter Chemistry, Anhui Key Laboratory of Optoelectronic Science and Technology, Department of Polymer Science and Engineering, University of Science and Technology of China, Hefei, 230026, China.
Max Planck Institute for Polymer Research, Ackermannweg 10, 55128, Mainz, Germany.
Small. 2022 Dec;18(52):e2205461. doi: 10.1002/smll.202205461. Epub 2022 Nov 11.
Metallodrugs are widely used in cancer treatment. The modification of metallodrugs with polyethylene glycol (PEGylation) prolongs blood circulation and improves drug accumulation in tumors; it represents a general strategy for drug delivery. However, PEGylation hinders cellular internalization and tumor penetration, which reduce therapeutic efficacy. Herein, the red-light-enhanced cellular internalization and tumor penetration of a PEGylated anticancer agent, PEGylated Ru complex (Ru-PEG), are reported upon. Ru-PEG contains a red-light-cleavable PEG ligand, anticancer Ru complex moiety, and fluorescent pyrene group for imaging and self-assembly. Ru-PEG self-assembles into vesicles that circulate in the bloodstream and accumulate in the tumors. Red-light irradiation induces dePEGylation and changes the Ru-PEG vesicles to large compound micelles with smaller diameters and higher zeta potentials, which enhance tumor penetration and cellular internalization. Red-light irradiation also generates intracellular O , which induces the death of cancer cells. This work presents a new strategy to enhance the cellular internalization and tumor penetration of anticancer agents for efficient phototherapy.
金属药物被广泛应用于癌症治疗。聚乙二醇（PEG）修饰金属药物可以延长血液循环时间并增加肿瘤内药物蓄积，这是一种常见的药物递送策略。然而，PEG 化会阻碍细胞内化和肿瘤穿透，从而降低治疗效果。在此，报道了一种聚乙二醇化抗癌剂聚乙二醇化钌配合物（Ru-PEG）的红光增强细胞内化和肿瘤穿透作用。Ru-PEG 含有可被红光裂解的聚乙二醇配体、抗癌的钌配合物部分和荧光苝基团，用于成像和自组装。Ru-PEG 自组装成囊泡，在血液中循环并在肿瘤中积累。红光照射诱导聚乙二醇的脱落，并将 Ru-PEG 囊泡转变为具有更小直径和更高 zeta 电位的大复合胶束，从而增强肿瘤穿透和细胞内化。红光照射还会产生细胞内的 O ，诱导癌细胞死亡。这项工作提出了一种新策略，可增强抗癌药物的细胞内化和肿瘤穿透作用，从而实现高效的光疗。
Macromol Biosci. 2025-6
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