Humanized bispecific antibody (mPEG × HER2) rapidly confers PEGylated nanoparticles tumor specificity for multimodality imaging in breast cancer

  • Yi-An Cheng (Creator)
  • Tung Ho Wu (Contributor)
  • Y. M. Wang (Contributor)
  • Tian Lu Cheng (Creator)
  • I. Ju Chen (Creator)
  • Yun-Chi Lu (Contributor)
  • Kuo-Hsiang Chuang (Contributor)
  • Chih Kuang Wang (Contributor)
  • Chiao Yun Chen (Creator)
  • Rui An Lin (Creator)
  • Huei Jen Chen (Creator)
  • Tzu Yi Liao (Contributor)
  • En Shuo Liu (Contributor)
  • Fang Ming Chen (Creator)



Abstract Background Developing a universal strategy to improve the specificity and sensitivity of PEGylated nanoaparticles (PEG-NPs) for assisting in the diagnosis of tumors is important in multimodality imaging. Here, we developed the anti-methoxypolyethylene glycol (mPEG) bispecific antibody (BsAb; mPEG × HER2), which has dual specificity for mPEG and human epidermal growth factor receptor 2 (HER2), with a diverse array of PEG-NPs to confer nanoparticles with HER2 specificity and stronger intensity. Result We used a one-step formulation to rapidly modify the nanoprobes with mPEG × HER2 and optimized the modified ratio of BsAbs on several PEG-NPs (Lipo-DiR, SPIO, Qdot and AuNP). The αHER2/PEG-NPs could specifically target MCF7/HER2 cells (HER2++) but not MCF7/neo1 cells (HER2+/−). The αHER2/Lipo-DiR and αHER2/SPIO could enhance the sensitivity of untargeted PEG-NPs on MCF7/HER2 (HER2++). In in vivo imaging, αHER2/Lipo-DiR and αHER2/SPIO increased the specific targeting and enhanced PEG-NPs accumulation at 175% and 187% on 24 h, respectively, in HER2-overexpressing tumors. Conclusion mPEG × HER2, therefore, provided a simple one-step formulation to confer HER2-specific targeting and enhanced sensitivity and contrast intensity on HER2 positive tumors for multimodality imaging.