Acylsulfonamide-Functionalized zwitterionic gold nanoparticles for enhanced cellular uptake at tumor pH

A nanoparticle design featuring pH-responsive alkoxyphenyl acylsulfonamide ligands is reported herein. As a result of ligand structure, this nanoparticle is neutral at pH 7.4, becoming positively charged at tumor pH (<6.5). The particle uptake and cytotoxicity increase over this pH range. This pH-controlled uptake and toxicity makes this particle a promising tool for tumor selective therapy. Tumor selective: A pH-responsive zwitterionic alkoxyphenyl acylsulfonamide ligand is used to functionalize the surface of gold nanoparticles (AuNPs) to form zwitterionic NPs. The NPs reversibly become cationic at tumor pH (<6.6) with concomitant enhancement of cellular uptake and cytotoxicity in tumor cells, providing scope for pH-controlled NP delivery.