Solubilization and anticancer-activity enhancement of Methotrexate by novel dendrimeric nanodevices synthesized in one-step reaction

The one-step synthesis of nanodevices based on PAMAM framework for targeted cancer therapy is described. Four water-soluble nanodevices (named fractions F1 to F4) were rightly separated by size discrimination, and characterized. From biological assays of cell growth inhibition percentage, the anticancer activity of Methotrexate (chemotherapeutic drug) as part of a nanodevice, generally increases over cancer cell lines and notably, in case of human lymphocytes, the cell growth inhibition percentage decreases drastically (more than 80%), thus, the nanodevices exhibited a favorable discrimination between healthy and diseased cells. From the characterization it can be conclude that the synthesized nanodevices provide a dual scenario of drug transportation: encapsulation and conjugation.

Dual scenario of drug transport Nanodevices containing MTX (anticancer drug) and FA (metabolite) were synthesized and tested in cell growth inhibition percentage assays. The nanodevices exhibited a favorable discrimination between healthy and diseased cells, against which there is a significant increase in the activity of MTX. A Dual transport behavior is attributed to these materials: conjugation and encapsulation.Figure optionsDownload as PowerPoint slideHighlights
► Novel dendrimeric nanodevices for cancer therapy were obtained in one-step synthesis.
► The synthesis of dendrimeric precursor (PAMAM-TRIS) was significantly optimized.
► Anticancer activity of MTX, as part of a nanodevice, increases over cancer cells.
► The nanodevices exhibit a positive discrimination between healthy and diseased cells.
► It is observed a dual scenario of drug transportation: encapsulation and conjugation.