Laboratory study reveals enhanced uptake and antitumor efficacy of Angiopep-2-conjugated nanoparticles in glioma models, indicating potential for brain-targeted drug delivery.
Key Points
To synthesize and evaluate fluorescently labeled Angiopep-2-conjugated PAMAM nanoparticles for targeted drug delivery across the blood-brain barrier and against glioma cells.
Angiopep-2 was conjugated to PAMAM dendrimers using MAL-PEG-NHS crosslinking and labeled with fluorescein isothiocyanate to yield FITC-APP nanoparticles.
In vitro cellular adhesion, uptake, transport, and cytotoxicity were assessed in brain microvascular endothelial cells, C6 glioma cells, and HEK-293 control cells.
In vivo antitumor efficacy was evaluated in animal glioma models in comparison with non-targeted FITC-PAMAM nanoparticles.
Synthesized FITC-APP nanoparticles exhibited an average hydrodynamic diameter of 32.23 ± 0.62 nm and a zeta potential of -4.36 ± 0.10 mV.
FITC-APP nanoparticles demonstrated significantly higher adhesion, uptake, and transport rates in brain endothelial and C6 glioma cells than non-targeted nanoparticles, with no significant differences in HEK-293 cells.
FITC-APP nanoparticles produced stronger C6 cell growth inhibition and superior antitumor responses in animal models compared to non-targeted controls.