Iguratimod encapsulated PLGA-NPs improves therapeutic outcome in glioma, glioma stem-like cells and temozolomide resistant glioma cells

Glioma is the most common neoplasm of the central nervous system, with the highest mortality rate. The present study was designed to examine the therapeutic effect of Iguratimod (IGU) encapsulated-poly (lactic-co-glycolic acid) PLGA nanoparticles (IGU-PLGA-NPs), which showed inhibition of glioma cells proliferation both in vitro and in vivo. IGU encapsulated in PLGA nanoparticles with an average size of 100-200 nm was prepared using modified double-emulsion (W1/O/W2) method. Cell Counting Kit-8 (CCK-8) analysis of Glioma cancer cells and glioma stem-like cells (GSCs) demonstrated significant inhibition of their growth treated with IGU-PLGA-NPs. IGU-PLGA-NPs inhibit migration in glioma cells as well as tumor sphere formation in GSCs. Treatment with IGU-PLGA-NPs showed a significant decrease in tumor growth through the apoptotic pathway in mice model without any visible organ toxicity and it can successfully cross the blood brain barrier (BBB). Most Importantly, IGU-PLGA-NPs significantly depleted growth of U251 Temozolomide-resistant (U251TMZ-R) cells. (C) 2019 Elsevier Inc. All rights reserved.