Abstract Objective To prepare α-(8-quinolinyloxy) monosubstituted phthalocyanine zinc nanosuspension (ZnPc-NS) for photodynamic therapy by intravenous administration. Methods The formulation and preparation technology of ZnPc-NS were assessed by particle size using the precipitation-high pressure homogenization method. The efficacy of ZnPc-NS was evaluated based on particle size, zeta potential, sedimentation ratio, TEM imaging, stability assessment, photodynamic activity and safety. Results and discussion The content, average particle size, polydispersity and photodegradation constant of ZnPc-NS were 0.2 mg/ml, 219.7 ± 7.41 nm, 0.19 ± 0.02 and 0.006, respectively. The photosensitization rate of singlet oxygen (1O2) of the ZnPc-NS was three times higher than that of the ZnPc DMF solution. ZnPc-NS exhibited optimal antitumor activity in HepG2 cells under light exposure and low photo- and non-light-associated toxicity in HELFX cells. In addition, low hemolysis and vascular stimulation were evident in the experiments performed. Conclusion The ZnPc-NS exhibited optimal stability, faster photosensitization rate of 1O2, and optimal antitumor activity and safety than the ZnPc DMF solution, which could provide potential support for further research and development.

中文翻译：

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一种用于潜在增强光动力疗法的新型 α-(8-喹啉氧基) 单取代锌酞菁纳米悬浮液

摘要 目的制备α-(8-喹啉氧基)单取代酞菁锌纳米混悬剂(ZnPc-NS)，用于静脉给药光动力治疗。方法采用沉淀-高压均质法，通过粒径对ZnPc-NS的配方和制备工艺进行评价。基于粒径、zeta 电位、沉降比、TEM 成像、稳定性评估、光动力活性和安全性评估 ZnPc-NS 的功效。结果与讨论 ZnPc-NS 的含量、平均粒径、多分散性和光降解常数分别为 0.2 mg/ml、219.7 ± 7.41 nm、0.19 ± 0.02 和 0.006。ZnPc-NS 的单线态氧 (1O2) 的光敏率是 ZnPc DMF 溶液的三倍。ZnPc-NS 在光照下在 HepG2 细胞中表现出最佳的抗肿瘤活性，在 HELFX 细胞中表现出低光相关和非光相关毒性。此外，在进行的实验中，低溶血和血管刺激是明显的。结论与ZnPc DMF溶液相比，ZnPc-NS表现出最佳的稳定性、更快的1O2光敏速率以及最佳的抗肿瘤活性和安全性，可为进一步的研究和开发提供潜在支持。