The antitumor activity of bismuth lipophilic nanoparticles (BisBAL NPs) on human glioblastoma is higher than temozolomide

Background: : Glioblastoma multiforme (GBM) is the most common type of brain tumor and it is considered as one of the most aggressive malignancies (1.5 years of survival rate). Objective: : Determine the antitumor potential of bismuth lipophilic nanoparticles (BisBAL NP) on a human glioblastoma cell-line. Methods: : BisBAL NP were characterized by scanning electron microscopy (SEM). BisBAL NP entry and intracellular distribution on U-87 MG cells were observed by transmission electron microscopy (TEM). The effect of BisBAL NP on tumor cells was evaluated by MTT assay (IC₅₀ value), Calcein AM staining, Live/dead assay, apoptosis quantification, and comet assay. Results: : BisBAL NP-induced cytotoxicity more efficient than temozolomide (TMZ). The IC₅₀ value of BisBAL NP was 12.7 µM. For the first time, direct interaction between BisBAL NP and plasmatic U-87 MG cell membrane was obtained by TEM. Calcein AM assay revealed loss of permeability of tumor cells after 24 h-exposure to 25 µM of BisBAL NP. 25 µM of BisBAL induced 48.5% of apoptosis, while 50 µM of BisBAL induced a higher rate of apoptosis 77.2%. Conclusion: : BisBAL NP inhibited U-87 MG cell growth through membrane attack and loss membrane permeability, apoptosis induction and later promoting genotoxicity among tumor cells.