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. Author manuscript; available in PMC: 2016 Jan 8.
Published in final edited form as: Acc Chem Res. 2012 Apr 30;45(11):1854–1865. doi: 10.1021/ar2003122

Figure 7. Antiestrogen gold nanoparticles for hormone receptor-targeted breast cancer treatment strategies.

Figure 7

(a) Illustration of 25 nm gold nanospheres conjugated with mixed self-assembled monolayers (SAMs) of a high molecular weight polymer stabilizer and a polymer-linked estrogen receptor antagonist, tamoxifen (TAM). Here, TAM acts as a combined targeting and therapeutic moiety which binds membrane- and cytoplasmic-estrogen receptor, inducing apoptosis. (b) High-density gold nanoparticle ligation dramatically accelerates drug influx rates via endocytosis of (104 TAM molecules per particle) versus passive diffusion of the free drug. (c) Optical dark-field scattering microscopy shows nanoparticle uptake into breast cancer cells in a receptor- and ligand-dependent manner. (d) Time-dependent dose-response kinetics show >104 enhanced drug potency from the targeted nanoparticle construct with up to 2.7-fold enhanced potency per equivalent tamoxifen molecule. Adapted with permission from Refs. 3,52. Copyright 2009 American Chemical Society and 2011 Royal Society of Chemistry.