Fibronectin extra domain B-specific aptide conjugated nanoparticles for targeted cancer imaging

Jinho Park, Sunghyun Kim, Phei Er Saw, In Hyun Lee, Mi Kyung Yu, Minsik Kim, Kwangyeol Lee, Yong Chul Kim, Yong Yeon Jeong, Sangyong Jon

Research output: Contribution to journalArticlepeer-review

40 Citations (Scopus)


Fibronectin extra domain B (EDB) is specifically expressed in cancer-associated blood vessels and extracellular matrix, and thus is a promising cancer biomarker. Very recently, we developed a novel class of high-affinity (< 100 nM) peptides, termed 'aptides', that specifically bind a variety of protein targets. Here, we describe superparamagnetic iron oxide nanoparticles (SPIONs) conjugated with EDB-specific aptides for use in targeted magnetic resonance imaging (MRI) of cancer. An anti-EDB aptide (APT EDB) containing an additional cysteine residue reacted with maleimide-terminated, PEGylated phospholipid (Mal-PEG2000-DSPE) to give an aptide-conjugated PEGylated phospholipid (APTEDB-PEG 2000-DSPE). A nanoemulsion method was then used to coat oleic acid-stabilized SPIONs with amphiphilic phospholipids, including APT EDB-PEG2000-DSPE, methoxy-PEG2000-DSPE, and rhodamine-DMPE. The resulting nanoparticles (APTEDB-SPIONs) had a hydrodynamic size of less than 50 nm and remained stable in an aqueous solution for at least 1 week. In in vitro studies, APTEDB-SPIONs showed specific uptake by EDB-overexpressing cell lines. In an in vivo Lewis lung carcinoma model that expresses a high level of the target EDB protein, MRI clearly revealed that APTEDB-SPIONs injected via the tail vein specifically accumulated at the tumor site. Non-targeting SPIONs lacking the anti-EDB aptide showed much lower uptake in tumor tissues than did aptide-conjugated nanoparticles. Further, we confirmed that the distribution of nanoparticles within the tumor tissue was well correlated with the areas where EDB was expressed. Our APTEDB-SPIONs hold high potential as a specific imaging modality for the detection of EDB-overexpressing tumors.

Original languageEnglish
Pages (from-to)111-118
Number of pages8
JournalJournal of Controlled Release
Issue number2
Publication statusPublished - 2012 Oct 28


  • Aptide
  • Cancer imaging
  • Fibronectin extra domain
  • MRI

ASJC Scopus subject areas

  • Pharmaceutical Science


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