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    Area of Science:

    • Nanotechnology
    • Materials Science
    • Oncology

    Background:

    • Development of theranostic nanoparticles for combined cancer therapy and diagnosis.
    • Diolein-based nanoparticles (DO-NPs) incorporating gadolinium complexes for MRI contrast.
    • Targeted delivery systems using folic acid conjugation for enhanced cellular uptake.

    Purpose of the Study:

    • To synthesize and characterize targeted theranostic nanoparticles (DO-NPs) for ovarian cancer treatment.
    • To evaluate the in vitro and in vivo efficacy of DO-NPs loaded with doxorubicin (DOX) and targeted with folic acid (FA).
    • To assess the theranostic capabilities, combining therapeutic effects with MRI imaging properties.

    Main Methods:

    • Synthesis of non-targeted DO-NPs with Gadolinium complex ((C18)2DTPA(Gd)) and targeted DO-NPs with varying amounts of (C18)2-Peg3000- FA.
    • In vitro studies including ICP-MS for Gadolinium quantification, Surface Plasmon Resonance (SPR) for cellular binding, cytotoxicity assays, and confocal microscopy.
    • In vivo studies using IGROV-1 tumor-bearing mice to evaluate antitumor effects via MRI imaging (T1w, T2w) and tumor growth regression.

    Main Results:

    • The formulation with 3% (C18)2-Peg3000- FA demonstrated the highest selectivity towards IGROV-1 cells.
    • Targeted DO-NPs loaded with DOX exhibited significant selective cytotoxicity and cellular uptake in IGROV-1 cells.
    • In vivo studies showed that DO-NP3-FA/DOX achieved 80% and 50% greater tumor growth regression compared to saline and Doxil, respectively.

    Conclusions:

    • Diolein-based nanoparticles functionalized with folic acid represent a promising targeted theranostic platform for cancer therapy.
    • The developed DO-NPs effectively combine the therapeutic action of doxorubicin with the diagnostic potential of gadolinium for MRI.
    • This study presents the first example of a targeted carrier with a stable foamy mesophase, offering superior therapeutic efficacy in preclinical models.