Yang Hui, Shang Zhanhao, Shi Qiankun, Gao Jucai, Wang Xiaorui, Hu Fang
Biomaterials Research Center, School of Biomedical Engineering, Southern Medical University, Guangzhou, 510515, China.
Microbiome Medicine Center, Department of Laboratory Medicine, Zhujiang Hospital, Southern Medical University, Guangzhou, 510515, China.
Chem Asian J. 2023 May 16;18(10):e202300212. doi: 10.1002/asia.202300212. Epub 2023 Apr 25.
Photodynamic therapy (PDT) is recognized to be a promising strategy for anticancer treatment. Considering the progressive application of PDT in clinical trials, highly efficient photosensitizers (PSs) are in strong demand. Aggregation-induced emission (AIE) based PSs are promising phototheranostic materials for tumor imaging and PDT due to their high fluorescence and photosensitizing efficiency. Herein, a PS, TPA-2BCP with AIE characteristics is developed by adopting an acceptor-π-donor-π-acceptor (A-π-D-π-A) structure. However, the accumulation of ionic PSs in the tumor is poor due to non-specific interactions with bio-molecules. Therefore, we use a carboxyl-rich polymer material, polyacrylate polyethylene glycol block copolymer (PEG-b-PAA) to encapsulate the cationic PSs into nanoparticles through ionic interactions. The cationic groups are blocked and the generated PS nanoparticles can accumulate well in the tumor site in vivo. Meanwhile, the photosensitizing efficiency of the PS is further enhanced in the nanoparticle format. The tumor growth can be obviously inhibited under 530 nm laser irradiation, demonstrating its potential application in antitumor PDT.
光动力疗法（PDT）被认为是一种很有前景的抗癌治疗策略。鉴于PDT在临床试验中的逐步应用，对高效光敏剂（PSs）的需求强烈。基于聚集诱导发光（AIE）的PSs因其高荧光和光敏效率，是用于肿瘤成像和PDT的有前景的光诊疗材料。在此，通过采用受体-π-供体-π-受体（A-π-D-π-A）结构开发了一种具有AIE特性的PS，即TPA-2BCP。然而，由于与生物分子的非特异性相互作用，离子型PSs在肿瘤中的积累较差。因此，我们使用富含羧基的聚合物材料聚丙烯酸酯聚乙二醇嵌段共聚物（PEG-b-PAA）通过离子相互作用将阳离子型PSs封装成纳米颗粒。阳离子基团被阻断，生成的PS纳米颗粒在体内能够很好地在肿瘤部位积累。同时，PS以纳米颗粒形式存在时其光敏效率进一步提高。在530nm激光照射下肿瘤生长可被明显抑制，证明了其在抗肿瘤PDT中的潜在应用。
