Abstract

Herein, a tumor-targeted multifunctional theranostic agent was synthetized using a facile method, combining four clinically approved materials: artesunate (Arte), human serum albumin (HSA), folic acid (FA), and indocyanine green (ICG). The obtained nanocomposites (FA-IHA NPs) showed an excellent photo- and physiological stability. The ICG in the FA-IHA NPs was used not only for near infrared (NIR) fluorescence imaging, but also for photothermal and photodynamic (PTT-PDT) therapy under a single NIR irradiation. In addition, the NIR irradiation (808 nm, 1 W/cm2) could trigger Arte release that showed enhanced chemotherapeutic effect. Through fluorescence imaging, the cell uptake and tumor accumulation of FA-IHA NPs were observed in vitro and in vivo, analyzed by confocal microscopy and NIR fluorescence imaging in tumor xenograft mice. Based on the diagnostic results, FA-IHA NPs at 24 h post injection and combined with NIR irradiation (808 nm, 1 W/cm2) could efficiently suppress tumor growth through a photo-chemo combination therapy, with no tumor recurrence in vitro and in vivo. The obtained results suggested that FA-IHA NPs are promising photo-chemo theranostic agents for future clinical translation.

Highlights

  • During these recent decades, imaging-guided photo-chemo therapy (IGPC) attracted great interest by many researchers, since it is a promising strategy to realize a personalized tumor therapy [1, 2]

  • We reported a targeted IGPC agent that covalently conjugated folic acid (FA) and indocyanine green (ICG) with human serum albumin (HSA) nanoparticles which encapsulated the anticancer drug artesunate (Arte) (FA-IHA NPs)

  • Synthesis and Characterization of FA-IHA NPs Artesunate was dissolved in DMSO and added into 15 mL water. 10 mg HSA powder was added into the above solution and stirred slightly for 3 h at room temperature

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Summary

Introduction

During these recent decades, imaging-guided photo-chemo therapy (IGPC) attracted great interest by many researchers, since it is a promising strategy to realize a personalized tumor therapy [1, 2]. IGPC allows the exact location of the tumor and traces the drug in vivo, guaranteeing an effective therapy and reducing side effects [3, 4]. IGPC should have the following characteristics: (i) a multifunctional theranostic agent with both imaging and therapeutic functions is needed; (ii) the theranostic agent should be biocompatible, stable, and specific against the tumor [5–8]. The imaging diagnosis modality in the IGPC usually includes magnetic resonance imaging, photoacoustic imaging, and fluorescence imaging [9–14]. Due to the high sensitivity, favorable temporal The IGPC combination could be a great strategy to overcome the above limitations

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