Methotrexate-Loaded PLGA Nanoparticles: Preparation, Characterization and their Cytotoxicity Effect on Human Glioblastoma U87MG Cells

Abstract

The purpose of the current study was to prepare Metho-trexate (MTX) loaded Poly Lactic-Co-Glycolic Acid (PLGA) Nanoparticles (NPs) and investigates their toxicity effect on human glioblastoma cells. The influence of different experimental parameters including polymer concentration, Polyvi-nyl Alcohol (PVA) concentration in the external phase and drug concentration on the particle size was evaluated. Size of NPs determined by Dynamic Light Scattering (DLS) and Scanning Electron Microscopy (SEM) was from 150 to 200 nm. The Encapsulation Efficiency (EE) and Drug Loading (DL) corresponding to the optimal conditions were 62.96% and 5.72%, respectively. Differential Scanning Calorimetric (DSC) and Fourier Transform Infrared Spectroscopy (FTIR) results indicated that MTX was dispersed as amorphous phase in the PLGA matrix and the chemical structure of MTX loaded PLGA did not change. Moreover, in vitro release profiles of MTX from NPs exhibited a sustained release behavior and the release rate of MTX from the NPs increased as the medium acidity enhanced. In vitro Cyto-toxicity studies revealed that the cell Cytotoxicity effect of MTX loaded PLGA NPs on U87MG cells was more than free MTX. In conclusion, MTX loaded PLGA NPs could be considered as potential candidate for drug delivery in the treatment of glioblastoma.