Design and Evaluation of the PLGA Nanoparticles Containing Ketorolac Tromethamine in Glioblastoma Treatment

The blood–brain barrier (BBB) separates blood from brain tissue, making drug delivery to the brain a significant challenge. This study aims to develop and optimize a novel nanoparticle system that may overcome the BBB and have a potential effect on glioblastoma. Ketorolac tromethamine (KT)-loaded poly(lactic-co-glycolic acid) (PLGA) RG 503-H nanoparticles were prepared using water/oil/water (W/O/W) emulsification solvent evaporation. KT-loaded nanoparticles have a particle size of 155.5 ± 2.08 nm, a zeta potential of -12.9 ± 1.23 mV, a polydispersity index of 0.111 ± 0.035, and an encapsulation efficiency of 53.46%. A significant portion of the drug (> 90%) was released in 6 h and completed within 24 h. When 3% (w/v) mannitol and trehalose were used as cryoprotectants, the nanoparticles remained physically stable. Additionally, it has been discovered that KT solution is cytotoxic at high doses to Rat Brain Glioblastoma (RG2) cells, and KT-loaded nanoparticles are more effective than drug solutions at lower doses. © The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature 2025.