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A Tumor-pH-Responsive Supramolecular Photosensitizer for Activatable Photodynamic Therapy with Minimal In Vivo Skin Phototoxicity
Theranostics ( IF 12.4 ) Pub Date : 2017-07-07 , DOI: 10.7150/thno.18861
Xingshu Li , Bi-Yuan Zheng , Mei-Rong Ke , Yongfan Zhang , Jian-Dong Huang , Juyoung Yoon

A major challenge in photodynamic therapy (PDT) is the development of new tumor-targeting photosensitizers. The tumor-specific activation is considered to be an effective strategy for designing these photosensitizers. Herein, we describe a novel tumor-pH-responsive supramolecular photosensitizer, LDH-ZnPcS8, which is not photoactive under neutral conditions but is precisely and efficiently activated in a slightly acidic environment (pH 6.5). LDH-ZnPcS8 is prepared by using a simple coprecipitation method based on the electrostatic interaction between negatively charged octasulfonate-modified zinc(II) phthalocyanine (ZnPcS8) and cationic hydroxide layers of layered double hydroxide (LDH). The in vitro photodynamic activities of LDH-ZnPcS8 in cancer cells are dramatically enhanced relative to those of ZnPcS8 alone. The results of in vivo fluorescence imaging demonstrate that the nanohybrid is activated in tumor tissues, where it displays an excellent PDT effect resulting in 95.3% tumor growth inhibition. Furthermore, the minimal skin phototoxicity of LDH-ZnPcS8 highlights its high potential as a novel photosensitizer for activatable PDT.

中文翻译:

肿瘤-pH响应性超分子光敏剂,用于可激活的光动力疗法,体内皮肤光毒性最小

光动力疗法(PDT)的主要挑战是开发新型靶向肿瘤的光敏剂。肿瘤特异性激活被认为是设计这些光敏剂的有效策略。在这里,我们描述了一种新型的肿瘤pH响应超分子光敏剂LDH-ZnPcS 8,它在中性条件下不具有光活性,但在微酸性环境(pH 6.5)中被精确有效地激活。LDH-ZnPcS 8是通过使用基于带负电荷的octasulfonate改性锌之间的静电相互作用的简单共沉淀法制备(II)酞菁(ZnPcS 8)和层状双氢氧化物(LDH)的阳离子的氢氧化层。在体外相对于单独的ZnPcS 8而言,LDH-ZnPcS 8在癌细胞中的光动力活性显着增强。体内荧光成像的结果表明,纳米杂交体在肿瘤组织中被激活,在纳米组织中显示出优异的PDT效果,导致95.3%的肿瘤生长抑制。此外,LDH-ZnPcS 8的最小皮肤光毒性突出了其作为可激活PDT的新型光敏剂的巨大潜力。
更新日期:2017-10-01
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