Methotrexate Gold Nanocarriers: Loading and Release Study: Its Activity in Colon and Lung Cancer Cells
Metadatos
Mostrar el registro completo del ítemAutor
Álvarez González, Beatriz; Rozalen, Marisa; Fernández Perales, María; Álvarez, Miguel A.; Sánchez Polo, ManuelEditorial
Mdpi
Materia
Au nanoparticles Nanocarriers Methotrexate Anticancer drug Chemotherapeutic Controlled release
Fecha
2020-12-21Referencia bibliográfica
Álvarez-González, B., Rozalen, M., Fernández-Perales, M., Álvarez, M. A., & Sánchez-Polo, M. (2020). Methotrexate Gold Nanocarriers: Loading and Release Study: Its Activity in Colon and Lung Cancer Cells. Molecules, 25(24), 6049. [doi:10.3390/molecules25246049]
Patrocinador
Spanish Government; Junta de Andalucía P18-RT-4193Resumen
In the present study, the synthesis of gold nanoparticles (AuNPs) loaded with methotrexate
(MTX) has been carried out in order to obtain controlled size and monodispersed nanocarriers of
around 20 nm. The characterization study shows metallic AuNPs with MTX polydispersed on
the surface. MTX is linked by the replacement of citrate by the MTX carboxyl group. The drug
release profiles show faster MTX release when it is conjugated, which leads to the best control of
plasma concentration. Moreover, the enhanced release observed at pH 5 could take advantage of
the pH gradients that exist in tumor microenvironments to achieve high local drug concentrations.
AuNP–MTX conjugates were tested by flow cytometry against lung (A-549) and colon (HTC-116)
cancer cell lines. Results for A-549 showed a weaker dose–response e ect than for colon cancer ones.
This could be related to the presence of folate receptors in line HTC-116 in comparison to line A-549,
supporting the specific uptake of folate-conjugated AuNP–MTX by folate receptor positive tumor
cells. Conjugates exhibited considerably higher cytotoxic e ects compared with the e ects of equal
doses of free MTX. Annexin V-PI tests sustained the cell death mechanism of apoptosis, which is
normally disabled in cancer cells.