Redox-responsive prodrug-like PEGylated macrophotosensitizer nanoparticles for enhanced near-infrared imaging-guided photodynamic therapy

• DOI: 10.1016/j.ejpb.2018.12.006
• Publication Date: 2018-12-11T03:53:28Z
• Authors: Zheng Ruan; Pan Yuan; Tuanwei Li; Youliang Tian; Quan Cheng; Lifeng Yan
• Keywords: Boron Compounds; Mice, Inbred BALB C; Photosensitizing Agents; Infrared Rays; Polymers; 01 natural sciences; Polyethylene Glycols; 0104 chemical sciences; Drug Liberation; Mice; Drug Delivery Systems; Photochemotherapy; Neoplasms; Animals; Humans; Nanoparticles; Female; Prodrugs; Particle Size; Hydrophobic and Hydrophilic Interactions; Oxidation-Reduction; Micelles

Efficient delivery of hydrophobic photosensitizer (PS) into tumor cells is a key step for photodynamic therapy (PDT). Redox-responsive polymeric nanoparticles of amphiphilic macro-photosensitizer has designed and prepared as a prodrug-like pro-photosensitizer (pro-PS) for PDT. PEG works as the hydrophilic block and the near infrared (NIR) brominated BODIPY derivative (BDP) works as the hydrophobic PS, and they were linked via the disulfide bond as PEG-SS-BDP, which could be broken for drug release owing to the high GSH concentration inside tumor cells. The amphiphilic PEG-SS-BDP can be self-assembled into polymeric micelles with suitable size (about 110 nm), which benefits prolonged blood circulation and enhanced tumor accumulation confirmed by NIR fluorescent imaging in vivo. The higher efficiency of PEG-SS-BDP nanoparticles (PSSBDP NPs) than non-responsive PDT agent (PEG-BDP) with similar structure was confirmed by both in vitro and in vivo studies, suggesting the advantages of the redox-responsive pro-PS system for improving potential near infrared tumor imaging and photodynamic therapy.