Synergistic Active Targeting to B16F10 Tumors by αvβ3/CD44-Targeted Nanoparticles Loaded with Docetaxel

  • Sanjun Shi
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


Generally, many drugs including nanomedicine can permeate into a superficial layer of tumors through an enhanced permeability and retention (EPR) effect. However, blood-tumor barrier negatively impacts permeation and accumulation of therapeutic drugs. The active targeting of nanoparticles to tumor endothelial cells (TECs) constitutes a breakthrough for overcoming this stint. Based on integrin αvβ3 (a highly specific TEC biomarker) and CD44 (a biomaker for tumor cells), a synergistic active targeting delivery system is able to target not only tumor blood vessels but also tumor cells. Therefore, a specific ligand of αvβ3, tetraiodothyroacetic acid (tetrac) and a major ligand of CD44, hyaluronan (HA), are employed to decorate on the surface of solid lipid nanoparticles (TeHA-SLNs). As a result, the docetaxel-loaded TeHA-SLNs (TeHA-SLNs/DTX) exhibit an excellent anti-tumor effect in vitro and in vivo through synergistic active-targeting function. This chapter gives an introduction to and discussion of the commonly used production and synthetic methods for tetrac conjugated HA and TeHA-SLNs/DTX. Moreover, the methods for characterization and cell targeting assessment in a αvβ3- and CD44-enriched B16F10 cell line are described. Finally, methods to assess targeting effects and antitumor activity of TeHA-SLNs/DTX in vivo are described.


CD44 Dual-targeting delivery system Integrin αvβ3 Nanoparticle Synergistic active targeting 



This work is supported by the project of the National Natural Science Foundation of China (81402876) and the Program for “1135” Excellent Talents in Daping Hospital. We also would like to thank Prof. Zhirong Zhang and Xun Sun from Sichuan University for providing B16F10 cell line.


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Copyright information

© Springer Science+Business Media New York 2018

Authors and Affiliations

  • Sanjun Shi
    • 1
  1. 1.Department of Pharmacy, Institute of Surgery Research, Daping HospitalThird Military Medical UniversityChongqingPeople’s Republic of China

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