Background: In the present study, the tumor-specific, pH-responsive peptide H₇K(R₂)₂ -modified, theranostic liposome-containing paclitaxel (PTX) and superparamagnetic iron oxide nanoparticles (SPIO NPs), PTX/SPIO-SSL-H₇K(R₂)₂, was prepared by using H₇K(R₂)₂ as the targeting ligand, SPIO NPs as the magnetic resonance imaging (MRI) agent, PTX as antitumor drug.
Methods: The PTX/SPIO-SSL-H₇K(R₂)₂ was prepared by a thin film hydration method. The characteristics of PTX/SPIO-SSL-H₇K(R₂)₂ were evaluated. The targeting effect, MRI, and antitumor activity of PTX/SPIO-SSL-H₇K(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 H₇K(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-H₇K(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.
Keywords: tumor-specific pH-responsive peptide, paclitaxel, superparamagnetic iron oxide nanoparticles, liposome, theranostic efficiency