Enhanced cytotoxic activity of bile acid cisplatin derivatives by conjugation with gold nanoparticles

•AuNPs can serve as carriers of platinum compounds.•Bile-acid cisplatin derivatives can be conjugated with AuNPs in a simple way.•MG-63 cells were tested.•Drug carriers conjugates show an enhanced cytotoxic activity.

This article explores the potential cytotoxic activity of bile-acid cisplatin derivatives like bisursodeoxycholate(ethylenediamine)platinum(II), PtU2, when conjugated with gold nanoparticles, being a promising alternative to cisplatin in the treatment of cancer due to their lower toxicity. For our purpose we analyzed the intracellular delivery ability of these compounds after conjugation with 20-nm gold nanoparticles (PtU2-AuNPs) in the MG63 (osteosarcoma) cell line. Same platinum uptake after incubation with PtU2 and PtU2-AuNPs-derivatives is associated with a higher cytotoxic activity in case of the platinum–gold nanoparticle conjugate, the overall IC50 of PtU2 being reduced more than 10 fold for these new conjugates. When conjugated with gold nanoparticles, this bile-acid derivative is more efficient than the platinum compound alone in terms of their cytotoxic activity.

Graphical abstractThis article reports results about preliminary cytotoxic activity studies of bile acid cisplatin derivatives loaded on gold nanoparticles carried into MG63 (osteosarcoma) cells.Figure optionsDownload full-size imageDownload as PowerPoint slide