Monoclonal antibody conjugated magnetic nanoparticles could target MUC-1-positive cells in vitro but not in vivo

MUC1 antigen is recognized as a high‐molecular‐weight glycoprotein that is unexpectedly over‐expressed in human breast and other carcinomas. In contrast, C595 a monoclonal antibody (mAb) against the protein core of the human urinary epithelial machine, is commonly expressed in breast carcinomas. The aim of this study was to conjugate ultra‐small super paramagnetic iron oxide nanoparticles (USPIO) with C595 mAb, in order to detect in vivo MUC1 expression. A dual contrast agent (the C595 antibody‐conjugated USPIO labeled with 99mTc) was prepared for targeted imaging and therapy of anti‐MUC1‐expressing cancers. The C595 antibody‐conjugated USPIO had good stability and reactivity in the presence of blood plasma at 37 °C. No significant differences were observed in immunoreactivity results between conjugated and nonconjugated nanoparticles. The T1 and T2 measurements show >79 and 29% increments (for 0.02 mg/ml iron concentrations) in T1 and T2 values for USPIO‐C595 in comparison with USPIO, respectively. The nanoprobes showed the interesting targeting capability of finding the MUC1‐positive cell line in vitro. However, we found disappointing in vivo results (i.e. very low accumulation of nanoprobes in the targeted site while >80% of the injected dose per gram was taken up by the liver and spleen), not only due to the coverage of targeting site by protein corona but also because of absorption of opsonin‐based proteins at the surface of nanoprobes. Copyright © 2014 John Wiley & Sons, Ltd. We obtained very promising in vitro results, but we found the in vivo results disappointing not only owing to the coverage of targeting site by protein corona but also because of absorption of opsonin‐based proteins at the surface of nanoprobes.