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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Cytotoxicity of Methotrexate Conjugated to Glycerol Phosphate Modified Superparamagnetic Iron Oxide Nanoparticles

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Deda, Daiana K. [1] ; Cardoso, Roberta M. [1] ; Kawassaki, Rodrigo K. [1] ; de Oliveira, Andre R. [1] ; Toma, Sergio H. [1] ; Baptista, Mauricio S. [2] ; Araki, Koiti [1]
Total Authors: 7
[1] Univ Sao Paulo, Dept Fundamental Chem, Inst Chem, Av Prof Lineu Prestes 748, BR-05508000 Sao Paulo, SP - Brazil
[2] Univ Sao Paulo, Inst Chem, Dept Biochem, Av Prof Lineu Prestes 748, BR-05508000 Sao Paulo, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Journal of Nanoscience and Nanotechnology; v. 21, n. 3, p. 1451-1461, MAR 2021.
Web of Science Citations: 0

A systematic study was carried out to evaluate the uptake and cytotoxicity of methotrexate (MTX) conjugated to superparamagnetic iron oxide nanoparticles (SPIONs) modified with glycerol phosphate (Glyc) and phosphorylethanolamine (PEA), using MCF-7 cancer cell line as model. The ligand shell composition was controlled in such a way to get SPIONs with nine different surface functionalization and up to three co-conjugated ligands but the very iron oxide core, in order to test and compare uptake and cytotoxicity, and verify possible additive effects. Folic acid (FA), the non-toxic analogue of MTX, was also explored as ligand for SPIONs. Glyc was shown to enhance dramatically the cellular uptake despite the high negative zeta potentials, whereas PEA, FA and MTX was found to have a much lower effect on the cellular uptake. Also, a significant ten times lowering of IC50 was observed for the co-conjugated MTX in the SPION-Glyc/PEA/MTX as compared to the free drug, whereas the analogue SPION-Glyc/PEA/FA nanoparticles exhibited no significant cytotoxicity. In short, the conjugation of MTX to SPIONs enhanced dramatically its cytotoxicity and decreased the IC50 value against MCF-7 tumor cells as compared to the free drug, probably due to the enhanced uptake of SPIONs as a result of their surface modification with Glyc/PEA, demonstrating that SPION-Glyc/PEA is a good nanocarrier for co-conjugated methotrexate. (AU)

FAPESP's process: 18/21489-1 - Supramolecular nanotechnology: design, materials and devices
Grantee:Henrique Eisi Toma
Support type: Research Projects - Thematic Grants
FAPESP's process: 19/02151-2 - Development of MRI and PET/PECT dual mode theranostic nanoagent
Grantee:Rodrigo Ken Kawassaki
Support type: Scholarships in Brazil - Doctorate (Direct)