John Garner

mPEG-PLGA and PLGA from PolySciTech used in development of nanoparticle therapy for brain cancer

Blog Post created by John Garner on Oct 16, 2018

Velpurisiva, 2018 glioblastoma PLGA polyscitecy.PNG

Glioblastoma is a common form of brain cancer which is typically fatal. The treatment of cancer requires the use of medicines that typically have very severe side-effects and a very narrow therapeutic window. Recently, a kinase inhibitor has shown promise for cancer therapy, however, it failed due to toxicity issues during phase 1 clinical trials. The ability to deliver this molecule in a more controlled manner may reduce the toxicity issues and allow for it to be used as a therapy. Recently, researchers from the University of Massachusetts and the Dana-Farber Cancer Institute used mPEG-PLGA (AK027) and PLGA (AP041) from PolySciTech ( to create nanoparticles loaded with a novel kinase inhibitor as a prototype therapy for brain-cancer. These nanoparticles allow for dosing smaller concentrations in a more time-controlled manner. This research holds promise to provide for improved therapies against this fatal disease. Read more: Velpurisiva, Praveena, Brandon Piel, Jack Lepine, and Prakash Rai. "GSK461364A, a Polo-Like Kinase-1 Inhibitor Encapsulated in Polymeric Nanoparticles for the Treatment of Glioblastoma Multiforme (GBM)." Bioengineering 5, no. 4 (2018): 83.


“Abstract: Glioblastoma Multiforme (GBM) is a common primary brain cancer with a poor prognosis and a median survival of less than 14 months. Current modes of treatment are associated with deleterious side effects that reduce the life span of the patients. Nanomedicine enables site-specific delivery of active pharmaceutical ingredients and facilitates entrapment inside the tumor. Polo-like kinase 1 (PLK-1) inhibitors have shown promising results in tumor cells. GSK461364A (GSK) is one such targeted inhibitor with reported toxicity issues in phase 1 clinical trials. We have demonstrated in our study that the action of GSK is time dependent across all concentrations. There is a distinct 15-20% decrease in cell viability via apoptosis in U87-MG cells dosed with GSK at low concentrations (within the nanomolar and lower micromolar range) compared to higher concentrations of the drug. Additionally, we have confirmed that PLGA-PEG nanoparticles (NPs) containing GSK have shown significant reduction in cell viability of tumor cells compared to their free equivalents. Thus, this polymeric nanoconstruct encapsulating GSK can be effective even at low concentrations and could improve the effectiveness of the drug while reducing side effects at the lower effective dose. This is the first study to report a PLK-1 inhibitor (GSK) encapsulated in a nanocarrier for cancer applications. Keywords: GSK461364A; Glioblastoma Multiforme; polymeric nanoparticles; cytotoxicity; enhanced permeability and retention; polo-like kinase inhibitor; oncology; oncomedicine; U-87 MG”