Research Article


2014, 7(9): 1291–1301


Gold nanorod–photosensitizer conjugate with extracellular pH-driven tumor targeting ability for photothermal/photodynamic therapy

Nannan Wang1,§, Zilong Zhao1,§, Yifan Lv1, Huanhuan Fan1, Huarong Bai1, Hongmin Meng1, Yuqian Long1, Ting Fu1, Xiaobing Zhang1, and Weihong Tan1,2 (*)

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1 Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio-Sensing and Chemometrics, College of Chemistry and Chemical Engineering, College of Biology, and Collaborative Research Center of Molecular Engineering for Theranostics, Hunan University, Changsha 410082, China
2 Department of Chemistry and Department of Physiology and Functional Genomics, Center for Research at Bio/nano Interface, Shands Cancer Center, UF Genetics Institute and McKnight Brain Institute, University of Florida, Gainesville, Florida 32611-7200, USA
§ These authors contributed equally to this work.

Keywords: photodynamic therapy, photothermal therapy, gold nanorods, targeting acidity, peptide
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Chlorin e6–pHLIPss–AuNRs, a gold nanorod–photosensitizer conjugate containing a pH (low) insertion peptide (pHLIP) with a disulfide bond which imparts extracellular pH (pHe)-driven tumor targeting ability, has been successfully developed for bimodal photodynamic and photothermal therapy. In this bimodal therapy, chlorin e6 (Ce6), a second-generation photosensitizer (PS), is used for photodynamic therapy (PDT). Gold nanorods (AuNRs) are used as a hyperthermia agent for photothermal therapy (PTT) and also as a nanocarrier and quencher of Ce6. pHLIPss is designed as a pHe-driven targeting probe to enhance accumulation of Ce6 and AuNRs in cancer cells at low pH. In Ce6– pHLIPss–AuNRs, Ce6 is close to and quenched by AuNRs, causing little PDT effect. When exposed to normal physiological pH 7.4, Ce6–pHLIPss–AuNRs loosely associate with the cell membrane. However, once exposed to acidic pH 6.2, pHLIP actively inserts into the cell membrane, and the conjugates are translocated into cells. When this occurs, Ce6 separates from the AuNRs as a result of disulfide bond cleavage caused by intracellular glutathione (GSH), and singlet oxygen is produced for PDT upon light irradiation. In addition, as individual PTT agent, AuNRs can enhance the accumulation of PSs in the tumor by the enhanced permeation and retention (EPR) effect. Therefore, as indicated by our data, when exposed to acidic pH, Ce6–pHLIPss–AuNRs can achieve synergistic PTT/PDT bimodality for cancer treatment.
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Gold nanorod–photosensitizer conjugate with extracellular pH-driven tumor targeting ability for photothermal/photodynamic therapy. Nano Res. 2014, 7(9): 1291–1301

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