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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Pluronic F127/carfilzomib-based nanomicelles as promising nanocarriers: synthesis, characterization, biological, and in silico evaluations
Journal of Molecular Liquids, Volume 346, Article 118271, Year 2022
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Description
In this work, we designed a drug delivery nanosystem based on oil-in-water Pluronic F127 nanomicelles to encapsulate and control the release of the antineoplasic drug carfilzomib (CFZ), and hypothesized that CFZ entrapment might result in a better effective and more localized cytotoxic effect on cancerous cells and to reduce its undesirable side effects for in vitro and in vivo applications. Pluronic F127/CFZ nanomicelles showed a high drug encapsulation efficiency (74.8%) and were allowed to achieve a sustained release pattern. Computational analyses were conducted to increase understanding of the nature and strength of mutual interactions between Pluronic F127 and CFZ. Simulation data indicated that the position of heteroatoms on CFZ influences the strength of attractive interactions in the Pluronic F127/CFZ nanomicelles. Cytotoxic activity of free and encapsulated CFZ was assayed in several cancerous cell lines, SHY-SY5Y human neuroblastoma, MCF7 breast, and HeLa cervical cancer cells employing the MTT colorimetric assay. We found that Pluronic F127/CFZ nanomicelles exhibited greater anti-proliferative activity than free CFZ (lower IC50s) and induced evident morphological alterations in cancer cells. Caspase-3 activity was assessed to determine the main mechanism of drug-induced cell death. Compared to free CFZ, our formulation only increased caspase-3 activity in HeLa cells. To examine the short-term toxicity of F127/CFZ nanomicelles, intravenous injections of free CFZ and F127/CFZ nanomicelles at three doses of 0.25 mg/kg, 0.5 mg/kg, and 1 mg/kg for five consecutive days were administered to an animal model. The potential anti-bactericidal activity of this new formulation was also assayed against four standard bacteria, including Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, and Enterococcus faecalis. Unfortunately, no significant bacteria-killing effects were detected despite other drugs of the same family showing promising results. Still, our new formulation showed desirable anti-cancer effects and might be a good therapeutic modality for cancer treatment. © 2021 Elsevier B.V.
Authors & Co-Authors
Rahdar, Abbas A.
Iran, Zabol
University of Zabol
Hajinezhad, Mohammad Reza
Iran, Zabol
University of Zabol
Sargazi, Saman
Iran, Zahedan
Zahedan University of Medical Sciences
Barani, Mahmood
Iran, Kerman
Kerman University of Medical Sciences
Taboada, Pablo
Spain, Santiago de Compostela
Universidad de Santiago de Compostela
Pandey, Sadanand
South Korea, Gyeongsan
Yeungnam University
Statistics
Citations: 20
Authors: 6
Affiliations: 6
Identifiers
Doi:
10.1016/j.molliq.2021.118271
ISSN:
01677322
Research Areas
Cancer
Environmental