In vivo tumor targeting and image-guided drug delivery with antibody-conjugated, radiolabeled mesoporous silica nanoparticles

Feng Chen, Hao Hong, Yin Zhang, Hector F. Valdovinos, Sixiang Shi, Glen S. Kwon, Charles P. Theuer, Todd E. Barnhart, Weibo Cai

Research output: Journal article publicationJournal articleAcademic researchpeer-review

265 Citations (Scopus)


Since the first use of biocompatible mesoporous silica (mSiO2) nanoparticles as drug delivery vehicles, in vivo tumor targeted imaging and enhanced anticancer drug delivery has remained a major challenge. In this work, we describe the development of functionalized mSiO2 nanoparticles for actively targeted positron emission tomography (PET) imaging and drug delivery in 4T1 murine breast tumor-bearing mice. Our structural design involves the synthesis, surface functionalization with thiol groups, PEGylation, TRC105 antibody (specific for CD105/endoglin) conjugation, and 64Cu-labeling of uniform 80 nm sized mSiO2 nanoparticles. Systematic in vivo tumor targeting studies clearly demonstrated that 64Cu-NOTA-mSiO 2-PEG-TRC105 could accumulate prominently at the 4T1 tumor site via both the enhanced permeability and retention effect and TRC105-mediated binding to tumor vasculature CD105. As a proof-of-concept, we also demonstrated successful enhanced tumor targeted delivery of doxorubicin (DOX) in 4T1 tumor-bearing mice after intravenous injection of DOX-loaded NOTA-mSiO 2-PEG-TRC105, which holds great potential for future image-guided drug delivery and targeted cancer therapy.

Original languageEnglish
Pages (from-to)9027-9039
Number of pages13
JournalACS Nano
Issue number10
Early online date1 Oct 2013
Publication statusPublished - 22 Oct 2013
Externally publishedYes


  • drug delivery
  • in vivo tumor targeting
  • mesoporous silica (mSiO) nanoparticles
  • positron emission tomography (PET)
  • theranostics
  • tumor angiogenesis

ASJC Scopus subject areas

  • Materials Science(all)
  • Engineering(all)
  • Physics and Astronomy(all)

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