These EGFR targeted nanoparticles exploit the overexpression of growth factor receptors in hypoxic, multidrug resistant cancer and inhibit the Warburg Effect by delivering Lonidamine (a hexokinase 2 inhibitor).  Lonidamine lowers the apoptotic threshold for paclitaxel and the drug combination reverses multidrug resistance in triple negative breast cancer.

SEM and ESCA of Non-targeted and EGFR-targeted Polymeric Nanoparticles.  The design of the targeting construct is also shown in Panel C.   ESCA analysis confirms targeting residue on surface of nanoparticles.

EGFR-targeted nanoparticles accumulate at the site of the tumor and have a similar biodistribution to non-targeted nanoparticles, yet have improved pharmacokinetics.

Targeted Nanoparticles Reduce Tumor Size and Reverse Drug Resistance.  Combination therapy (lonidamine and paclitaxel) with EGFR-targeted nanoparticles reduce tumor size and reduce the expression of EGFR, HIF, HXK2, P-gp, and SCF.

Treatment with EGFR-Targeted Nanoparticles Improves Plasma Pharmacokinetics.

Treatment with EGFR-Targeted Nanoparticles Improves Tumor Pharmacokinetics.