A novel α-(8-quinolinyloxy) monosubstituted zinc phthalocyanine nanosuspension for potential enhanced photodynamic therapy

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.

Keywords:

• Phthalocyanine zinc
• nanosuspension
• photodegradation
• singlet oxygen
• photodynamic therapy

Disclosure statement

No potential conflict of interest was reported by the author(s).

Author contributions

Xiaqin Fang, An Xie, Hui Song, Dong Jiang, He Li, Zhiqiang Wang, Xiaochuan Tan, Yujia Zhang, Aiping Wang and Wensheng Zheng participated in conducting the study. Wensheng Zheng, Xiaqin Fang and Hui Song designed and performed the majority of the study. All other authors also contributed to data analysis. Xiaqin Fang, An Xie, Hui Song drafted the manuscript. Dong Jiang, He Li provided language help and with writing assistance. Wensheng Zheng proofread the article. All other authors amended the manuscript and agreed to publication.

Additional information

Funding

This work was supported by the CAMS Innovation Fund for Medical Sciences (No.2017-I2M-1-011,No.2017-I2M-3-012),The drug Innovation Major Project (No. 2018ZX09721003-007-007, No.2018ZX09721003-008-018, No.2018ZX09721003-008-019).