A facile strategy to enable nanoparticles for simultaneous phase transfer, folate receptor targeting, and cisplatin delivery

Abstract

Diagnostic and therapeutic strategies related to cancer treatment are being continually developed for enhancing the effectiveness of the treatment. Active targeting nanoparticles (NPs) with therapeutic capability are a major requirement of cancer therapeutics. Herein, we present a general one-pot approach for simultaneously (1) achieving the phase transfer of various NPs from an organic solvent to an aqueous phase, and (2) grafting an active targeting ligand (folate) via electrostatic interactions as well as a therapeutic agent (cisplatin) via coordinative interactions of platinum atoms with carboxylic acid ligands on the surface of the NPs. This approach allows rapid, simple, and versatile bioconjugation without the need for additional crosslinking reagents. Taking AgInS₂/ZnS quantum dots (AQDs) as an example, we show that NPs can be tailored to possess both targeting activity and therapeutic capability. In this study, AQDs exhibited a dose-dependent antiproliferative effect on HeLa cancer cells, indicating the possibility of using the obtained AQDs as highly effective dual-modality imaging probes for simultaneous cancer diagnosis and chemotherapy. In addition, the proposed one-pot approach can be extended to various other NPs (e.g., quantum dots, metal oxides, and metallic and magnetic materials) that can be successfully conjugated with folate via hydrophobic interactions and electrostatic immobilization during ultrasonication. Bioconjugation of the NPs was investigated by dynamic light scattering, ultraviolet-visible spectroscopy, and Fourier transform infrared spectroscopy before and after the phase transfer.