Methotrexate-conjugated quantum dots: synthesis, characterisation and cytotoxicity in drug resistant cancer cells

• DOI: 10.3109/1061186x.2015.1058801
• Publication Date: 2015-07-15T13:47:33Z
• Authors: Mohammad Johari-Ahar; Jaleh Barar; Ali Mohammad Aliz...; Soodabeh Davaran; Yadollah Omidi; Mohammad-Reza Ras...
• Keywords: Folate receptor; Conjugate

Methotrexate (MTX), a folic acid derivative, is potent anticancer used for treatment of different malignancies, but possible initiation drug resistance to MTX by cancer cells has limited its applications. Nanoconjugates (NCs) quantum dots (QDs) may favour the cellular uptake via folate receptors (FRs)-mediated endocytosis that circumvents efflux functions cells. We synthesised MTX-conjugated l-cysteine capped CdSe QDs (MTX-QD nanoconjugates) and evaluated their internalisation cytotoxicity in KB with/without resistancy MTX. The NCs were fully characterised high resolution transmission electron microscopy (HR-TEM), atomic force (AFM), dynamic light scattering (DLS) optical spectroscopy. Upon conjugation with MTX, photoluminescence (PL) properties altered, while an obvious quenching PL was observed after physical mixing. MTX-QD nanoconjugates efficiently internalised into cells, induced markedly (IC50, 12.0 µg/mL) MTX-resistant as compared free molecules (IC50,105.0 µg/mL), whereas, these values respectively about 7.0 0.6 µg/mL MTX-sensitive Based on findings, are proposed targeted therapy cancers, which provide improved outcome relapsed FR-overexpressing cancers.