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Evaluation of novel platinum(ii) based AIE compound-encapsulated mesoporous silica nanoparticles for cancer

Sheik Saleem Pasha1, Leena Fageria, Clàudia Climent

  • 1Department of Chemistry, Pilani Campus, BITS, Pilani, Rajasthan 333031, India. ir_laskar@pilani.bits-pilani.ac.in.

Dalton Transactions (Cambridge, England : 2003)
|March 9, 2018
PubMed

Insights

Researchers developed a novel platinum(II) molecule with aggregation-induced emission (AIE) properties for cancer theranostics. This molecule, BMPP-Pt, shows potent cytotoxicity and intracellular fluorescence, paving the way for single-compound cancer monitoring and treatment.

Area of Science:

  • Biomedical Engineering
  • Materials Science
  • Oncology

Background:

  • Cancer is a complex, heterogeneous disease requiring continuous therapy monitoring.
  • Existing theranostic agents have limitations like poor resolution, radiation damage, and high costs.
  • A single-molecule approach for simultaneous cancer diagnosis and therapy is highly desirable.

Purpose of the Study:

  • To design and synthesize a novel platinum(II)-based aggregation-induced emission (AIE) molecule for cancer theranostics.
  • To evaluate the dual functionality of the AIE molecule (BMPP-Pt) for intracellular fluorescence and cytotoxic activity.
  • To enhance cancer cell targeting and therapeutic efficacy using mesoporous silica nanoparticles (MSNPs) and aptamer functionalization.

Main Methods:

  • Synthesis and characterization of a novel platinum(II)-based AIE molecule (BMPP-Pt).
  • Encapsulation of BMPP-Pt into mesoporous silica nanoparticles (Pt-MSNPs).
  • Surface modification of Pt-MSNPs with anti-EpCAM aptamer (Pt-MSNP-E) for targeted delivery.

Main Results:

  • BMPP-Pt demonstrated strong intracellular fluorescence (emission maxima at 497 nm) and potent cytotoxic activity.
  • Pt-MSNP-E exhibited enhanced cytotoxicity and intracellular fluorescence compared to unmodified Pt-MSNPs and free BMPP-Pt.
  • Both BMPP-Pt and its nanoparticle formulations induced cancer cell death via apoptosis, potentially through G1 phase cell cycle arrest.

Conclusions:

  • EpCAM-functionalized BMPP-Pt loaded MSNPs show efficient internalization and apoptosis induction in cancer cells.
  • The developed theranostic system displays strong intracellular fluorescence, enabling simultaneous imaging and therapy.
  • This study presents a promising single-compound based theranostic modality for future cancer treatment strategies.

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