GAGomers are lipid nanoparticles coated with the glycosaminoglycan (GAG) hyaluronan (HA). A wide range of therapeutic molecules can be integrated into the lipid core. Since HA is a carbohydrate native to the human body, it can act as a non-immunogenic biocompatible coating that shields the core and the therapeutic payload while providing targeting and delivery into tumor cells.
Selective targeting and active cellular uptake of the GAGomers is achieved by cooperative avidity-driven binding of the HA coating the surface of the GAGomers by overexpressed, activated receptors on the cell surface. The overexpression of activated HA receptors on the tumor cells is acquired during evolution of the tumor, differentiating these cells from normal tissues. GAGomers are engineered to take optimal advantage of this tumor characteristic.
A549 Tumor cells take-up GAGomers
Normal Human Keratinocytes do not
Time-elapsed video of fluorescently-labeled GAGomers (red) exposed to cells over 30 minutes.