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Cyclic Peptide-Gadolinium Nanoparticles for Enhanced Intracellular Delivery
Content Provider | MDPI |
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Author | Shirazi, Amir Park, Shang Rad, Shirin Baloyan, Luiza Mandal, Dindyal Sajid, Muhammad Hall, Ryley Lohan, Sandeep Zoghebi, Khalid Parang, Keykavous Tiwari, Rakesh |
Copyright Year | 2020 |
Description | A cyclic peptide containing one cysteine and five alternating tryptophan and arginine amino acids [(WR)5C] was synthesized using Fmoc/tBu solid-phase methodology. The ability of the synthesized cyclic peptide to produce gadolinium nanoparticles through an in situ one-pot mixing of an aqueous solution of GdCl3 with [(WR)5C] peptide solution was evaluated. Transmission electron microscopy showed the formed peptide-Gd nanoparticles in star-shape morphology with a size of ~250 nm. Flow cytometry investigation showed that the cellular uptake of a cell-impermeable fluorescence-labeled phosphopeptide (F′-GpYEEI, where F′ = fluorescein) was approximately six times higher in the presence of [(WR)5C]-Gd nanoparticles than those of F′-GpYEEI alone in human leukemia adenocarcinoma (CCRF-CEM) cells after 2 h incubation. The antiproliferative activities of cisplatin and carboplatin (5 µM) were increased in the presence of [(WR)5C]-GdNPs (50 μM) by 41% and 18%, respectively, after 72-h incubation in CCRF-CEM cells. The intracellular release of epirubicin, an anticancer drug, from the complex showed that 15% and 60% of the drug was released intracellularly within 12 and 48 h, respectively. This report provides insight about using a non-toxic MRI agent, gadolinium nanoparticles, for the delivery of various types of molecular cargos. |
Starting Page | 792 |
e-ISSN | 19994923 |
DOI | 10.3390/pharmaceutics12090792 |
Journal | Pharmaceutics |
Issue Number | 9 |
Volume Number | 12 |
Language | English |
Publisher | MDPI |
Publisher Date | 2020-08-21 |
Access Restriction | Open |
Subject Keyword | Pharmaceutics Medicinal Chemistry Drug Delivery Systems Cyclic Peptides Gadolinium Nanoparticles Intracellular Transportation Nanocarriers |
Content Type | Text |
Resource Type | Article |