1. 99m Tc-doxorubicin-loaded gallic acid-gold nanoparticles ( 99m Tc-DOX-loaded GA-Au NPs) as a multifunctional theranostic agent.
- Author
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El-Ghareb WI, Swidan MM, Ibrahim IT, Abd El-Bary A, Tadros MI, and Sakr TM
- Subjects
- Animals, Antibiotics, Antineoplastic administration & dosage, Breast Neoplasms drug therapy, Cell Line, Tumor, Doxorubicin administration & dosage, Drug Carriers chemistry, Drug Delivery Systems, Female, Gold chemistry, Humans, Inhibitory Concentration 50, MCF-7 Cells, Mice, Particle Size, Precision Medicine, Technetium chemistry, Antibiotics, Antineoplastic pharmacology, Doxorubicin pharmacology, Gallic Acid chemistry, Metal Nanoparticles
- Abstract
The development of cancer theranostic nanomedicines is recommended to concurrently achieve and evaluate the therapeutic benefit and progress. The current work aims to develop gallic acid-gold nanoparticles (GA-Au NPs) as a theranostic probe for
99m Tc-Doxorubicin (99m Tc-DOX) based on the spatiotemporal release pattern induced intra-tumoral (IT) delivery. DOX-loaded GA-Au NPs were developed and identified via UV-Vis spectroscopy. The system was characterized for drug loading efficiency%, particle size, zeta potential, topography, in vitro DOX release and anti-proliferative activity against the MCF-7 cell-line. The factors influencing radiolabeling efficiency of DOX with99m Tc (DOX concentration, stannous chloride concentration, reaction time and pH) were optimized. The in vitro stability in mice serum and in vivo distribution studies in mice of99m Tc-DOX-loaded GA-Au NPs were investigated following IV and IT administration. Dox-loaded GA-Au NPs had a loading efficiency of 91%, a small particle size (≈50 nm), a promising zeta potential (-20 mV) and a sustained drug release profile at pH 5.3. GA-Au NPs exhibited increased anti-proliferative activity, with approximately a four-fold lower IC50 value (0.15 μg/ml) than free DOX. The optimized radiolabeling efficiency of99m Tc-DOX was ≈93%. It showed good physiological stability in mice serum for at least 8 h. The IT delivery of99m Tc-DOX-loaded GA-Au NPs in tumor-induced mice showed dramatic tumor accumulation. A maximum magnitude of 86.73%ID/g was achieved, at 15 min post-injection, with a target/non-target ratio of ≈56.99m Tc-DOX-loaded GA-Au NPs could be used for the selective IT delivery of a chemotherapeutic agent and an imaging agent to a target organ., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier B.V. All rights reserved.)- Published
- 2020
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