Jeong, Keunsoo Park, Solji Lee, Yong-Deok Kang, Chi Soo Kim, Hyun Jun Park, Hyeonjong Kwon, Ick Chan Kim, Jungahn Park, Chong Rae Kim, Sehoon 2024-01-20T03:33:45Z 2024-01-20T03:33:45Z 2021-09-05 2016-08-01 0927-7765 https://pubs.kist.re.kr/handle/201004/123801 Current approaches in use of water-insoluble photosensitizers for photodynamic therapy (PDT) of cancer often demand a nano-delivery system. Here, we report a photosensitizer-loaded biocompatible nano delivery formulation (PPaN-20) whose size was engineered to ca. 20 nm to offer improved cell/tissue penetration and efficient generation of cytotoxic singlet oxygen. PPaN-20 was fabricated through the physical assembly of all biocompatible constituents: pyropheophorbide-a (PPa, water-insoluble photo sensitizer), polycaprolactone (PCL, hydrophobic/biodegradable polymer), and Pluronic F-68 (clinically approved polymeric surfactant). Repeated microemulsification/evaporation method resulted in a fine colloidal dispersion of PPaN-20 in water, where the particulate PCL matrix containing well-dispersed PPa molecules inside was stabilized by the Pluronic corona. Compared to a control sample of large-sized nanoparticles (PPaN-200) prepared by a conventional solvent displacement method, PPaN-20 revealed optimal singlet oxygen generation and efficient cellular uptake by virtue of the suitably engineered size and constitution, leading to high in vitro phototoxicity against cancer cells. Upon administration to tumor bearing mice by peritumoral route, PPaN-20 showed efficient tumor accumulation by the enhanced cell/tissue penetration evidenced by in vivo near-infrared fluorescence imaging. The in vivo PDT treatment with peritumorally administrated PPaN-20 showed significantly enhanced suppression of tumor growth compared to the control group, demonstrating great potential as a biocompatible photosensitizing agent for locoregional PDT treatment of cancer. (C) 2016 Elsevier B.V. All rights reserved. English ELSEVIER SCIENCE BV SINGLET OXYGEN GENERATION NANOPARTICLES DELIVERY PHOTOSENSITIZER Size-engineered biocompatible polymeric nanophotosensitizer for locoregional photodynamic therapy of cancer Article 10.1016/j.colsurfb.2016.04.029 1 COLLOIDS AND SURFACES B-BIOINTERFACES, v.144, pp.303 - 310 COLLOIDS AND SURFACES B-BIOINTERFACES 144 303 310 scie scopus 000377837200035 2-s2.0-84971596784 Biophysics Chemistry, Physical Materials Science, Biomaterials Biophysics Chemistry Materials Science Article SINGLET OXYGEN GENERATION NANOPARTICLES DELIVERY PHOTOSENSITIZER Pyropheophorbide-a Polycaprolactone Pluronic polymer nanoparticle Physical assembly Photodynamic therapy