Theranostic unimolecular micelles based on brush-shaped amphiphilic block copolymers for tumor-targeted drug delivery and positron emission tomography imaging

Jintang Guo, Hao Hong, Guojun Chen, Sixiang Shi, Tapas R. Nayak, Charles P. Theuer, Todd E. Barnhart, Weibo Cai, Shaoqin Gong

Research output: Journal article publicationReview articleAcademic researchpeer-review

67 Citations (Scopus)


Brush-shaped amphiphilic block copolymers were conjugated with a monoclonal antibody against CD105 (i.e., TRC105) and a macrocyclic chelator for 64Cu-labeling to generate multifunctional theranostic unimolecular micelles. The backbone of the brush-shaped amphiphilic block copolymer was poly(2-hydroxyethyl methacrylate) (PHEMA) and the side chains were poly(l-lactide)-poly(ethylene glycol) (PLLA-PEG). The doxorubicin (DOX)-loaded unimolecular micelles showed a pH-dependent drug release profile and a uniform size distribution. A significantly higher cellular uptake of TRC105-conjugated micelles was observed in CD105-positive human umbilical vein endothelial cells (HUVEC) than nontargeted micelles due to CD105-mediated endocytosis. In contrast, similar and extremely low cellular uptake of both targeted and nontargeted micelles was observed in MCF-7 human breast cancer cells (CD105-negative). The difference between the in vivo tumor accumulation of 64Cu-labeled TRC105-conjugated micelles and that of nontargeted micelles was studied in 4T1 murine breast tumor-bearing mice, by serial positron emission tomography (PET) imaging and validated by biodistribution studies. These multifunctional unimolecular micelles offer pH-responsive drug release, noninvasive PET imaging capability, together with both passive and active tumor-targeting abilities, thus making them a desirable nanoplatform for cancer theranostics.

Original languageEnglish
Pages (from-to)21769-21779
Number of pages11
JournalACS Applied Materials and Interfaces
Issue number24
Early online date14 Mar 2014
Publication statusPublished - 24 Dec 2014
Externally publishedYes


  • Cu
  • angiogenesis
  • brush polymer
  • brush-shaped amphiphilic block copolymer
  • cancer
  • CD105
  • nanocarriers
  • positron emission tomography (PET)
  • theranostics
  • unimolecular micelles

ASJC Scopus subject areas

  • Materials Science(all)

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