The theranostic efficiency of tumor-specific, pH-responsive, peptide-modified, liposome-containing paclitaxel and superparamagnetic iron oxide nanoparticles.

Background: In the present study, the tumor-specific, pH-responsive peptide H7 K(R2 )2 -modified, theranostic liposome-containing paclitaxel (PTX) and superparamagnetic iron oxide nanoparticles (SPIO NPs), PTX/SPIO-SSL-H7 K(R2 )2 , was prepared by using H7 K(R2 )2 as the targeting ligand, SPIO NPs as the magnetic resonance imaging (MRI) agent, PTX as antitumor drug.

Methods: The PTX/SPIO-SSL-H7 K(R2 )2 was prepared by a thin film hydration method. The characteristics of PTX/SPIO-SSL-H7 K(R2 )2 were evaluated. The targeting effect, MRI, and antitumor activity of PTX/SPIO-SSL-H7 K(R2 )2 were investigated detail in vitro and in vivo in human breast carcinoma MDA-MB-231 cell models.

Results: Our results of in vitro flow cytometry, in vivo imaging, and in vivo MR imaging confirmed the pH-responsive characteristic of H7 K(R2 )2 in MDA-MB-231 cell line in vitro and in vivo. The results of in vivo MRI and in vivo antitumor activity confirmed the theranostic effect of PTX/SPIO-SSL-H7 K(R2 )2 in MDA-MB-231 tumor-bearing model.

Conclusion: Considering all our in vitro and in vivo results, we conclude that we developed targeting modified theranostic liposome which could achieve both role of antitumor and MRI.