Image-guided and tumor-targeted drug delivery with radiolabeled unimolecular micelles

Jintang Guo, Hao Hong, Guojun Chen, Sixiang Shi, Qifeng Zheng, Yin Zhang, Charles P. Theuer, Todd E. Barnhart, Weibo Cai, Shaoqin Gong

Research output: Journal article publicationJournal articleAcademic researchpeer-review

82 Citations (Scopus)


Unimolecular micelles formed by dendritic amphiphilic block copolymers poly(amidoamine)-poly(l-lactide)-b-poly(ethylene glycol) conjugated with anti-CD105 monoclonal antibody (TRC105) and 1,4,7-triazacyclononane-N, N', N-triacetic acid (NOTA, a macrocyclic chelator for 64Cu) (abbreviated as PAMAM-PLA-b-PEG-TRC105) were synthesized and characterized. Doxorubicin (DOX), a model anti-cancer drug, was loaded into the hydrophobic core of the unimolecular micelles formed by PAMAM and PLA via physical encapsulation. The unimolecular micelles exhibited a uniform size distribution and pH-sensitive drug release behavior. TRC105-conjugated unimolecular micelles showed a CD105-associated cellular uptake in human umbilical vein endothelial cells (HUVEC) compared with non-targeted unimolecular micelles, which was further validated by cellular uptake in CD105-negative MCF-7 cells. In 4T1 murine breast tumor-bearing mice, 64Cu-labeled targeted micelles exhibited a much higher level of tumor accumulation than 64Cu-labeled non-targeted micelles, measured by serial non-invasive positron emission tomography (PET) imaging and confirmed by biodistribution studies. These unimolecular micelles formed by dendritic amphiphilic block copolymers that synergistically integrate passive and active tumor-targeting abilities with pH-controlled drug release and PET imaging capabilities provide the basis for future cancer theranostics.

Original languageEnglish
Pages (from-to)8323-8332
Number of pages10
Issue number33
Early online date8 Aug 2013
Publication statusPublished - Nov 2013
Externally publishedYes


  • CD105 (endoglin)
  • Dendritic amphiphilic block copolymer
  • Molecular imaging
  • Nanocarriers
  • Positron emission tomography (PET)
  • Unimolecular micelles

ASJC Scopus subject areas

  • Bioengineering
  • Ceramics and Composites
  • Biophysics
  • Biomaterials
  • Mechanics of Materials


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