Self-Remedied Nanomedicine for Surmounting the Achilles’ Heel of Photodynamic Tumor Therapy

• DOI: 10.1021/acsabm.1c00938
• Publication Date: 2021-10-21T00:40:33Z
• Authors: Xiang Zhou; Jia-Qi Huang; Ling-Shan Liu; Fu-An Deng; Yi-Bin Liu; Yan-Mei Li; A-Li Chen; Xi-Yong Yu; Shi-Ying Li; Hong Cheng
• Keywords: Hypoxia; Tumor Hypoxia

Oxygen-dependent photodynamic therapy (PDT) could exacerbate tumor hypoxia to induce the upregulation of hypoxia-inducible factor-1α (HIF-1α), which would promote growth and metastasis. In this paper, a self-remedied nanomedicine is developed based on photosensitizer HIF-1α inhibitor surmount Achilles' heel PDT for enhanced antitumor efficacy. Specifically, (designated as CYC-1) prepared by self-assembly chlorine e6 (Ce6) 3-(5′-hydroxy-methyl-2′-furyl)-1-benzylindazole (YC-1) through π–π stacking hydrophobic interactions. Of special note, carrier-free CYC-1 holds an extremely high drug loading rate avoids excipient-triggered adverse reactions. Intravenously administered prefers accumulate in tissue effective cellular uptake. More importantly, it verified that capable inhibiting activity, thereby improving its efficacy suppression. Besides, has overwhelming superiority restraining proliferation over combined administration Ce6 YC-1, highlights advantage strategy delivery therapy. This study sheds light development self-delivery efficient against malignancies.