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Surface-engineered core-shell upconversion nanoparticles for effective hypericin delivery and multimodal imaging.

Taras Vasylyshyn1, Veronika Huntošová2,3, Vitalii Patsula1

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This study introduces novel upconversion nanoparticles (UCNPs) for targeted hypericin (Hyp) delivery to tumors. These UCNPs enhance photodynamic therapy efficacy and show promise for future cancer treatment applications.

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Area of Science:

  • Nanotechnology
  • Materials Science
  • Biomedical Engineering

Background:

  • Nanotechnology accelerates cancer diagnosis and treatment.
  • Upconversion nanoparticles (UCNPs) show potential in drug delivery and tumor imaging.
  • Targeted delivery of photosensitizers is crucial for effective photodynamic therapy.

Purpose of the Study:

  • To develop a novel UCNP-based delivery system for the photosensitizer hypericin (Hyp) into malignant tumors.
  • To enhance the photodynamic therapy (PDT) efficacy using UCNPs for targeted cancer treatment.
  • To evaluate the safety and efficacy of the developed nanoparticle system.

Main Methods:

  • Synthesis of core-shell NaYF4:Yb3+,Er3+@NaYF4:Nd3+ UCNPs via thermal decomposition.
  • Coating UCNPs with poly(N,N-dimethylacrylamide-co-2-aminoethyl acrylate)-alendronate [P(DMA-AEA)-Ale] for stability.
  • Conjugation of hypericin (Hyp) to the UCNP system and validation using multimodal imaging and MTT assays.

Main Results:

  • Successfully synthesized and characterized UCNP-based nanoparticles loaded with Hyp.
  • Validated nanoparticle internalization in Jurkat cells using multimodal imaging techniques.
  • Demonstrated enhanced photodynamic effect and significant cancer cell viability reduction post-irradiation compared to Hyp alone.
  • Confirmed Hyp release is higher in acidic tumor environments, indicating tumor-specific drug delivery.

Conclusions:

  • The developed UCNP@P(DMA-AEA)-Ale-Hyp system is a promising platform for targeted hypericin delivery and enhanced photodynamic cancer therapy.
  • The nanoparticles exhibit good stability, cellular uptake, and therapeutic efficacy with minimal cytotoxicity.
  • The tumor-specific release profile suggests suitability for future in vivo applications in cancer treatment.