Targeted drug delivery via human epidermal growth factor receptor for sustained release of allyl isothiocyanate

In this study, allyl-isothiocyanate (AITC)-loaded Polylactic-Co-Glycolic Acid (PLGA) Nanoparticles (NPs) were prepared for targeting epithelial squamous carcinoma cells using a specific antibody targeting the Epidermal Growth Factor (EGF) receptor overexpressed on the cell membranes. AITC-loaded PLGA NPs showed more effective anticancer properties compared with free AITC, and their cytotoxicity was even more pronounced when the anti-EGFR antibody was covalently attached to the NPs surface. This targeting ability was additionally tested by co-culturing cervical HeLa cells, with very few EGFR on the membranes, and epithelial squamous carcinoma A431 cells, which largely overexpressed EFGR, being observed the specific localization of the antibody-functionalized AITC-loaded PLGA NPs solely in the latter types of cells, whereas non-functionalized NPs were distributed randomly in both cell types in much lesser extents. Thus, our findings support the development of drug delivery strategies that enhances the delivery of anti-cancer natural compounds to tumor tissue, in this case, by targeting specific tumor cell receptors with cell-specific ligands followed by tumor sensitization.