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 H(7)K(R(2))(2)-modified, theranostic liposome-containing paclitaxel (PTX) and superparamagnetic iron oxide nanoparticles (SPIO NPs), PTX/SPIO-SSL-H(7)K(R(2))(2), was prepared by using H(7)K(R(2))(2) as the targeting ligand, SPIO NPs as the magnetic resonance imaging (MRI) agent, PTX as antitumor drug. METHODS: The PTX/SPIO-SSL-H(7)K(R(2))(2) was prepared by a thin film hydration method. The characteristics of PTX/SPIO-SSL-H(7)K(R(2))(2) were evaluated. The targeting effect, MRI, and antitumor activity of PTX/SPIO-SSL-H(7)K(R(2))(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 H(7)K(R(2))(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-H(7)K(R(2))(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.