Methotrexate loaded on magnetite iron nanoparticles coated with chitosan: Biosynthesis, characterization, and impact on human breast cancer MCF-7 cell line.

PMID 30172815 | DOI 10.1016/j.ijbiomac.2018.08.118 · International journal of biological macromolecules · 2018 · View on PubMed ↗

Methotrexate (MTX) is effective therapeutic agent treated many tumors and autoimmune diseases. The aim of our study was to design an effective delivery nanocarrier for methotrexate to improve stability and biodistribution, reduce adverse effects and maximize clinical efficacy. Magnetite nanoparticles (Fe3O4-NPs) were synthesized using Pterocladiella. The size of Fe3O4-NPs, CS-Fe3O4-NPs and MTX/CS-Fe3O4-NPs were 37.6, 61.4 and 150 nm respectively. Methotrexate loading efficiency was 74.15% of total amount of MTX loaded on CS-Fe3O4-NPs and 39.8% of the loaded drug was initially released and the remaining amount was released through 120 h. The IC50 of MTX and MTX/CS-Fe3O4-NPs was 51.4 and 9.7 μg/ml respectively after 72 h. MTX/CS-Fe3O4-NPs caused remarkable damage to the membrane of MCF-7 cells led to increasing the LDH activity 5 fold in MCF-7 cells as compared with MTX treated once. DNA fragmentation and caspase-3 activity were higher in MCF-7 cells treated with MTX/CS-Fe3O4-NPs than that of MTX. Up-regulation of caspase3 and DHFR genes expression was observed in the treatment with MTX/CS-Fe3O4-NPs. The loading of MTX on chitosan coated Fe3O4-NPs improves the release and anticancer efficacy of MTX for effective cancer treatment.