A Self‐Transformable pH‐Driven Membrane‐Anchoring Photosensitizer for Effective Photodynamic Therapy to Inhibit Tumor Growth and Metastasis

• DOI: 10.1002/adfm.201702122
• Publication Date: 2017-07-31T11:00:36Z
• Authors: Guo‐Feng Luo; Wei‐Hai Chen; Sheng Hong; Qian Cheng; Wen‐Xiu Qiu; Xian‐Zheng Zhang
• Keywords: Cell membrane

Poor tumor selectivity and short life span of reactive oxygen species (ROS) are two major challenges in photodynamic therapy (PDT). In this study, a self‐transformable pH‐driven membrane anchoring photosensitizer (pHMAPS) is used to realize tumor‐specific accumulation situ PDT on cell maximize the therapeutic potency. It found that pHMAPS was able form α‐helix structure under acidic condition (pH 6.5 or 5.5), while remain random coil at normal pH 7.4. This secondary switch enables successful insertion into lipid bilayer, especially for cancerous microenvironment. Under laser irradiation, cytotoxic ROS generated immediate vicinity membrane, resulting superior killing effect vitro significant inhibition growth vivo. Importantly, benefited from membrane‐specific PDT, growth‐induced hepatic, pulmonary, as well osseous metastases breast cancer cells also retarded after treatment. Thus, localized by provides simple but effective strategy enhance medical performance photosensitizing agents therapy.