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Cyclic Peptide-Gadolinium Nanoparticles for Enhanced Intracellular Delivery
Amir Nasrolahi Shirazi1, Shang Eun Park2, Shirin Rad1
1Department of Pharmaceutical Sciences, College of Pharmacy, Marshall B. Ketchum University, Fullerton, CA 92831, USA.
Pharmaceutics
|August 23, 2020
Summary
Researchers synthesized gadolinium nanoparticles using a cyclic peptide [(WR)5C]. These peptide-Gd nanoparticles enhance cellular uptake and drug delivery, showing potential as a non-toxic MRI contrast agent for targeted cancer therapy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Medicinal Chemistry
Background:
- Gadolinium nanoparticles (GdNPs) are promising non-toxic MRI contrast agents.
- Peptide-based synthesis offers a novel approach for nanoparticle fabrication.
- Targeted drug delivery systems are crucial for improving cancer therapy efficacy.
Purpose of the Study:
- To synthesize and characterize gadolinium nanoparticles using a cyclic peptide [(WR)5C].
- To evaluate the potential of these peptide-Gd nanoparticles for enhanced cellular uptake and drug delivery.
- To explore their application as a non-toxic MRI agent in cancer treatment.
Main Methods:
- Solid-phase peptide synthesis of [(WR)5C].
- In situ synthesis of GdNPs via one-pot mixing of GdCl3 and peptide solution.
- Characterization using Transmission Electron Microscopy (TEM) and Flow Cytometry.
- Evaluation of cellular uptake, antiproliferative activity, and drug release kinetics.
Main Results:
- Star-shaped peptide-Gd nanoparticles (~250 nm) were successfully synthesized.
- Cellular uptake of a phosphopeptide was six times higher with peptide-Gd nanoparticles.
- Antiproliferative effects of cisplatin and carboplatin were significantly enhanced.
- Intracellular release of epirubicin reached 60% within 48 hours.
Conclusions:
- [(WR)5C]-Gd nanoparticles are effectively synthesized and exhibit star-shaped morphology.
- These nanoparticles enhance cellular uptake and drug delivery, improving anticancer drug efficacy.
- The developed peptide-Gd nanoparticles show potential as non-toxic MRI agents for targeted cancer therapy and molecular cargo delivery.

