HER2-specific aptide conjugated magneto-nanoclusters for potential breast cancer imaging and therapy

Jinho Park, Seho Park, Sunghyun Kim, In Hyun Lee, Phei Er Saw, Kwangyeol Lee, Yong Chul Kim, Young Joon Kim, Omid C. Farokhzad, Yong Yeon Jeong, Sangyong Jon

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)


Here, we report a nanotheranostic system that enables simultaneous imaging and therapy of HER2-overexpressing tumors. We first screened an aptide-based phage library for HER2-specific peptide ligands, identifying a HER2-specific aptide (APTHER2) phage clone. Chemically synthesized APT HER2 showed high affinity for its target protein (Kd ≈ 89 nM) and specifically bound HER2-overexpressing cells (NIH3T6.7) and tumor tissue slices. Next, we prepared HER2-specific-aptide-conjugated magneto-nanoclusters (APTHER2-MNCs) by a rehydration method using oleic acid-stabilized superparamagnetic iron oxide nanoparticles (SPIONs) and amphiphilic phospholipids, yielding nanoparticles with a hydrodynamic diameter of 47 ± 10 nm. The APTHER2-MNCs showed higher transverse (r2) relaxivity (∼180 mM-1 s-1) and greater drug-loading capacity compared to the equivalent isolated SPIONs (∼120 mM-1 s-1). When intravenously injected into HER2-overexpressing NIH3T6.7 tumor-bearing mice, APTHER2-MNCs substantially accumulated in tumor tissue, enhancing the relative signal by ∼45% at 3 h post-injection. This allowed us to detect the tumor using magnetic resonance imaging. Furthermore, after docetaxel loading, the drug-loaded APTHER2-MNCs remarkably inhibited the growth of HER2-overexpressing tumors (∼50% relative to controls) with little apparent toxicity, measured as changes in body weight. Together, these results indicate that APTHER2-MNCs show promise as an efficient nanotheranostic system that enables specific cancer imaging as well as targeted therapy.

Original languageEnglish
Pages (from-to)4576-4583
Number of pages8
JournalJournal of Materials Chemistry B
Issue number36
Publication statusPublished - 2013 Sept 28

ASJC Scopus subject areas

  • Chemistry(all)
  • Biomedical Engineering
  • Materials Science(all)


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