Ling Bo, Wang Yaguang, Dong Huaze, Chen Hongqi, Wang Lun
Department of Chemistry and Pharmaceutical Engineering, Hefei Normal University Hefei 230061 China.
Anhui Province Key Laboratory of Biomedical Materials and Chemical Measurement, Key Laboratory of Functional Molecular Solids, Ministry of Education, College of Chemistry and Materials Science, Anhui Normal University Wuhu 241002 China
Nanoscale Adv. 2025 Apr 7;7(10):3068-3076. doi: 10.1039/d4na01050g. eCollection 2025 May 13.
A core-shell-shell nanoplatform responsive to alkaline phosphatase (ALP) was developed for efficient tumor targeting and near-infrared (NIR)-activated photodynamic therapy (PDT). Specifically, UCNP@SiO-Bodipy@FFYp was synthesized by encapsulating upconversion nanoparticles (UCNPs) within a silica shell, embedding bodipy derivatives as photosensitizers, and covalently attaching a phosphorylated peptide (FFYp). Förster resonance energy transfer (FRET) from the UCNP emission at 550 nm to bodipy facilitated reactive oxygen species (ROS) generation upon NIR excitation. In the tumor microenvironment, ALP-triggered dephosphorylation converted UCNP@SiO-Bodipy@FFYp into the more hydrophobic UCNP@SiO-Bodipy@FFY, thereby promoting tumor cell uptake and tumor-specific accumulation. By leveraging this ALP-responsive targeting strategy alongside the deep-tissue penetration of NIR light, significant tumor growth inhibition was achieved both and . Notably, after 15 days of treatment in Balb/c mice bearing HeLa tumors, the tumor volume was reduced by over 95%. Taken together, these results highlight the promise of UCNP@SiO-Bodipy@FFYp as a tumor-responsive nanoplatform for highly effective, targeted PDT in cancer therapy.
开发了一种对碱性磷酸酶（ALP）有响应的核壳壳型纳米平台，用于高效肿瘤靶向和近红外（NIR）激活的光动力疗法（PDT）。具体而言，通过将上转换纳米粒子（UCNPs）包裹在二氧化硅壳内、嵌入硼二吡咯衍生物作为光敏剂并共价连接磷酸化肽（FFYp）来合成UCNP@SiO-Bodipy@FFYp。在近红外激发下，从UCNP在550nm处的发射到硼二吡咯的荧光共振能量转移（FRET）促进了活性氧（ROS）的产生。在肿瘤微环境中，ALP触发的去磷酸化将UCNP@SiO-Bodipy@FFYp转化为疏水性更强的UCNP@SiO-Bodipy@FFY，从而促进肿瘤细胞摄取和肿瘤特异性积累。通过利用这种对ALP有响应的靶向策略以及近红外光的深部组织穿透能力，在[具体条件1]和[具体条件2]下均实现了显著的肿瘤生长抑制。值得注意的是，在携带HeLa肿瘤的Balb/c小鼠中治疗15天后，肿瘤体积减少了超过95%。综上所述，这些结果突出了UCNP@SiO-Bodipy@FFYp作为一种肿瘤响应型纳米平台在癌症治疗中用于高效、靶向PDT的前景。
