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Production and Targeting of Monovalent Quantum Dots
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Targeting of somatostatin receptors expressed in blood cells using quantum dots coated with vapreotide

Ahmed A H Abdellatif1,2, Heba A Abou-Taleb3, Ahmed A Abd El Ghany4

  • 1Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt.

Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society
|December 12, 2018
PubMed

Insights

Quantum dots (Qdots) coated with vapreotide (VAP) show promise for targeted cancer therapy. This VAP-conjugated Qdots approach enhances drug delivery and imaging for improved cancer treatment outcomes.

Area of Science:

  • Nanotechnology in Medicine
  • Bioconjugation Chemistry
  • Cancer Therapeutics

Background:

  • Targeting cancer remains a significant challenge in effective treatment.
  • Quantum dots (Qdots) offer potential for targeted drug delivery and imaging.
  • Vapreotide (VAP), a somatostatin receptors (SSTRs) agonist, can be utilized for cancer cell targeting.

Purpose of the Study:

  • To develop and characterize Qdots coated with VAP (Qdots-VAP) for active cancer cell targeting.
  • To evaluate the efficacy of Qdots-VAP for cancer cell imaging and therapeutic outcome improvement.
  • To assess the cellular uptake and in vivo distribution of Qdots-VAP.

Main Methods:

  • Conjugation of VAP to Qdots using an amine-to-sulfhydryl crosslinker.
  • Characterization of Qdots-VAP via size determination, zeta potential measurement, and UV fluorometry.
  • Assessment of cellular uptake using confocal microscopy and flow cytometry in different cell lines.
  • In vivo study involving injection of Qdots-VAP into a rat model.

Main Results:

  • Qdots-VAP exhibited a size of 604.88 ± 17 nm, with a shift in zeta potential indicating successful VAP conjugation.
  • Fluorometry showed a redshift for Qdots-VAP compared to unmodified Qdots.
  • High specific binding and cellular uptake of Qdots-VAP were observed in SSTRs-expressing cells (17.3 MFU vs. 3.1 MFU control, P < 0.001).
  • In vivo studies demonstrated significant accumulation of Qdots-VAP in blood cells (70%).

Conclusions:

  • Qdots-VAP demonstrates efficient active targeting of cancer cells expressing SSTRs.
  • The developed Qdots-VAP system enhances drug delivery and improves therapeutic outcomes.
  • Qdots-VAP holds potential for cancer diagnosis and treatment, particularly for blood cell diseases.
Keywords:
BloodQuantum dotsReceptorSomatostatinTargetingVapreotide

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