NIR Imaging-Guided Photothermal Therapy by cRGD-Conjugated Solid Lipid Nanoparticles Encapsulating IR-780

  • Ye Kuang
  • Kunchi Zhang
  • Min Liu
  • Renjun PeiEmail author
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


It is extremely demanded to enhance the accumulation of near-infrared theranostic agents in the tumor region, which is favorable to the effective phototherapy. Compared with indocyanine green (a clinically applied dye), IR-780 iodide possesses higher and more stable fluorescence intensity and can be utilized as an imaging-guided PTT agent with laser irradiation. However, lipophilicity and short circulation time limit its applications in cancer imaging and therapy. Moreover, solid lipid nanoparticles (SLNs) conjugated with c(RGDyK) were designed as efficient carriers to improve the targeted delivery of IR-780 to the tumors. The multifunctional cRGD-IR-780 SLNs exhibited a desirable monodispersity, preferable stability, and significant targeting to cell lines over-expressing α v β 3 integrin. Additionally, the in vitro assays such as cell viability and in vivo PTT treatment denoted that U87MG cells or U87MG transplantation tumors could be eradicated by applying cRGD-IR-780 SLNs under the laser irradiation. Therefore, the resulted cRGD-IR-780 SLNs may serve as a promising NIR imaging-guided targeting PTT agent for cancer therapy. In this methodological chapter, we present the general flowchart applied for this project: (1) the synthesis of cRGD-IR-780 SLNs, (2) the physico-chemical characterization of the nanoparticles, (3) the cellular uptake and in vitro photothermal toxicity of the nanoparticles, and (4) the in vivo evaluation of the nanoparticles for NIR Imaging-guided PTT.


c(RGDyK) Imaging-guided therapy IR-780 dye Near-infrared Photothermal therapy Solid lipid nanoparticles 



This work was financially supported by the Natural Science Foundation of China (21575154, 21507156), the Natural Science Foundation of Jiangsu Province (BK20161262), the Science and Technology Foundation of Suzhou (SYG201526), and the CAS/SAFEA International Innovation Teams program.


  1. 1.
    Vahrmeijer AL, Hutteman M, van der Vorst JR et al (2013) Image-guided cancer surgery using near-infrared fluorescence. Nat Rev Clin Oncol 10(9):507–518CrossRefGoogle Scholar
  2. 2.
    Yan L, Qiu L (2015) Indocyanine green targeted micelles with improved stability for near-infrared image-guided photothermal tumor therapy. Nanomedicine 10(3):361–373CrossRefGoogle Scholar
  3. 3.
    Peng CL, Shih YH, Lee PC et al (2011) Multimodal image-guided photothermal therapy mediated by 188Re-labeled micelles containing a cyanine-type photosensitizer. ACS Nano 5(7):5594–5607CrossRefGoogle Scholar
  4. 4.
    Yan F, Wu H, Liu HM et al (2016) Molecular imaging-guided photothermal/photodynamic therapy against tumor by iRGD-modified indocyanine green nanoparticles. J Controlled Release 224:217–228CrossRefGoogle Scholar
  5. 5.
    Gianella A, Jarzyna PA, Mani V et al (2011) Multifunctional nanoemulsion platform for imaging guided therapy evaluated in experimental cancer. ACS Nano 5(6):4422–4433CrossRefGoogle Scholar
  6. 6.
    Zhang D, Wu M, Zeng Y et al (2015) Chlorin e6 conjugated poly(dopamine) nanospheres as PDT/PTT dual-modal therapeutic agents for enhanced cancer therapy. ACS Appl Mater Interfaces 7(15):8176–8187CrossRefGoogle Scholar
  7. 7.
    Zeng Y, Zhang D, Wu M et al (2014) Lipid-AuNps@ PDA nanohybrid for MRI/CT imaging and photothermal therapy of hepatocellular carcinoma. ACS Appl Mater Interfaces 6(16):14266–14277CrossRefGoogle Scholar
  8. 8.
    Chen YJ, Li ZH, Wang HB et al (2016) IR-780 Lloaded phospholipid mimicking homopolymeric micelles for near-IR imaging and photothermal therapy of pancreatic cancer. ACS Appl Mater Interfaces 8(11):6852–6858CrossRefGoogle Scholar
  9. 9.
    Jiang C, Cheng H, Yuan A et al (2015) Hydrophobic IR780 encapsulated in biodegradable human serum albumin nanoparticles for photothermal and photodynamic therapy. Acta Biomater 14:61–69CrossRefGoogle Scholar
  10. 10.
    Fu G, Zhu L, Yang K et al (2016) Diffusion-weighted magnetic resonance imaging for therapy response monitoring and early treatment prediction of photothermal therapy. ACS Appl Mater Interfaces 8(8):5137–5147CrossRefGoogle Scholar
  11. 11.
    Yue CX, Liu P, Zheng MB et al (2013) IR-780 dye loaded tumor targeting theranostic nanoparticles for NIR imaging and photothermal therapy. Biomaterials 34(28):6853–6861CrossRefGoogle Scholar
  12. 12.
    Zheng M, Yue C, Ma Y et al (2013) Single-step assembly of DOX/ICG loaded lipid—polymer nanoparticles for highly effective chemo-photothermal combination therapy. ACS Nano 7(3):2056–2067CrossRefGoogle Scholar
  13. 13.
    Sahu A, Lee JH, Lee HG et al (2016) Prussian blue/serum albumin/indocyanine green as a multifunctional nanotheranostic agent for bimodal imaging guided laser mediated combinatorial phototherapy. J Controlled Release 236:90–99CrossRefGoogle Scholar
  14. 14.
    Kulbacka J, Pucek A, Kotulska M et al (2016) Electroporation and lipid nanoparticles with cyanine IR-780 and flavonoids as efficient vectors to enhanced drug delivery in colon cancer. Bioelectrochemistry 110:19–31CrossRefGoogle Scholar
  15. 15.
    Kuo YC, Ko HF (2013) Targeting delivery of saquinavir to the brain using 83-14 monoclonal antibody-grafted solid lipid nanoparticles. Biomaterials 34(20):4818–4830CrossRefGoogle Scholar
  16. 16.
    Han YQ, Zhang P, Chen YY et al (2014) Co-delivery of plasmid DNA and doxorubicin by solid lipid nanoparticles for lung cancer therapy. Int J Mol Med 34(1):191–196CrossRefGoogle Scholar
  17. 17.
    Luo Y, Yang J, Yan Y et al (2015) RGD-functionalized ultrasmall iron oxide nanoparticles for targeted T(1)-weighted MR imaging of gliomas. Nanoscale 7(34):14538–14546CrossRefGoogle Scholar
  18. 18.
    Kuang Y, Zhang KC, Cao Y et al (2017) Hydrophobic IR-780 dye encapsulated in cRGD-conjugated solid lipid nanoparticles for NIR imaging-guided photothermal therapy. ACS Appl Mater Interfaces 9(14):12217–12226CrossRefGoogle Scholar

Copyright information

© Springer Science+Business Media New York 2018

Authors and Affiliations

  1. 1.CAS Key Laboratory of Nano-Bio Interface, Division of NanobiomedicineSuzhou Institute of Nano-Tech and Nano-Bionics, Chinese Academy of SciencesSuzhouChina
  2. 2.Shanghai University of Medicine and Health SciencesShanghaiChina

Personalised recommendations