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Mater Sci Eng C Mater Biol Appl. 2016 Oct 1;67:611-622. doi: 10.1016/j.msec.2016.05.047. Epub 2016 May 16.

Enhanced cellular uptake and phototoxicity of Verteporfin-conjugated gold nanoparticles as theranostic nanocarriers for targeted photodynamic therapy and imaging of cancers.

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Tianjin Key Laboratory for Photoelectric Materials and Devices, School of Materials Science & Engineering, Tianjin University of Technology, Tianjin 300384, PR China; Graduate School of Energy Science and Technology, Chungnam National University, Daejeon 305-764, South Korea.
Department of Nanobiomedical Science, Dankook University Graduate School, Cheonan 330-714, South Korea; Institute of Tissue Regeneration Engineering (ITREN) & College of Dentistry, Dankook University, Cheonan 330-714, South Korea.
Department of Biomedical Science, College of Medicine, Dankook University, Cheonan, 330-714, South Korea.
Graduate School of Energy Science and Technology, Chungnam National University, Daejeon 305-764, South Korea; Department of Chemical Engineering Education, College of Education, Chungnam National University, Daejeon 305-764, South Korea. Electronic address:


Activatable theranostics with the capacity to respond to a given stimulus have recently been intensively explored to develop more specific, individualized therapies for various diseases, and to combine diagnostic and therapeutic capabilities into a single agent. In this work, we designed tumor-targeting ligand-conjugated block copolymer-gold nanoparticle (AuNP) conjugates as multifunctional nanocarriers of the hydrophobic photosensitizer (PS), verteporfin (Verte), for simultaneous photodynamic therapy and imaging of cancers. Folic acid (FA)-conjugated block copolymers composed of polyethylene glycol (PEG) and poly-β-benzyl-l-aspartate (PBLA) were attached to citrate-stabilized AuNPs through a bidentate dihydrolipoic acid (DHLA) linker. The resulting AuNP conjugates (FA-PEG-P(Asp-Hyd)-DHLA-AuNPs) were significantly more stable than unmodified AuNPs, and their optical properties were not affected by pH. The hydrophobic PS, Verte, was covalently incorporated onto the surfaces of the AuNP conjugates through a pH-sensitive linkage, which increased the water solubility of Verte from <1μg/ml to >2000μg/ml. The size of FA-PEG-P(Asp-Hyd)-DHLA-AuNPs-Verte as determined by light-scattering measurements was about 110.3nm, and FE-SEM and FE-TEM images showed that these nanoparticles were spherical and showed adequate dispersivity after modification. In particular, an in vitro cell study revealed high intracellular uptake of FA-PEG-P(Asp-Hyd)-DHLA-AuNPs-Verte (about 98.62%) and marked phototoxicity after laser irradiation compared with free Verte. These results suggest that FA-PEG-P(Asp-Hyd)-DHLA-AuNPs-Verte has great potential as an effective nanocarrier for dual imaging and photodynamic therapy.


Gold nanoparticles; Imaging; Photodynamic therapy; Theranostics; Verteporfin

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