Phthalocyanine-based photosensitizer with tumor-pH-responsive properties for cancer theranostics. Issue 38 (10th September 2018)

• Record Type: Journal Article
• Authors: Yan, Shufeng; Chen, Jincan; Cai, Liangzhi; Xu, Peng; Zhang, Yaxin; Li, Shijie; Hu, Ping; Chen, Xueyuan; Huang, Mingdong; Chen, Zhuo
• Is Part Of: Journal of materials chemistry. Volume 6:Issue 38(2018)
• Page Start: 6080
• Page End: 6088
• Publication Date: 2018-09-10
• Subjects: Materials -- Periodicals; Chemistry, Analytic -- Periodicals; Biomedical materials -- Research -- Periodicals; 543.0284
• DOI: 10.1039/c8tb01884g
• Languages: English
• ISSNs: 2050-750X

Abstract

Abstract : A versatile phthalocyanine-based photosensitizer with tumor-pH-responsive properties for cancer theranostics. Abstract : Photodynamic therapy (PDT) has attracted attention for its potential for tumor destruction. We herein report a pH-responsive photosensitizer, synthesized by conjugating zinc phthalocyanine (ZnPc) with 2, 4, 6-tris( N, N -dimethylaminomethyl) phenoxy (TAP), which exhibited high phototoxicity at pH 6.5 (slightly acidic condition as in the extracellular tumor microenvironment) but no obvious phototoxicity at physiological pH 7.4. This pH-responsive photosensitizer specifically destroyed mouse mammary carcinoma cells 4T1 with an IC50 of 0.20 μM under a relatively low light dosage (2.5 J cm −2 ). The subsequent in vivo studies using 4T1-bearing mice demonstrated that this tumor-targeting photosensitizer ZnPc(TAP)4 not only ablated tumor cells photodynamically but also presented clear fluorescence cell imaging of tumor sites. These findings suggest that such a tumor-pH-responsive photosensitizer based on phthalocyanine may open up a new avenue for tumor-targeted and image-guided cancer theranostics in PDT.