Glyco-Nanovesicles with Activatable Near-Infrared Probes for Real-Time Monitoring of Drug Release and Targeted Delivery

A glyco-nanovesicle (Lac-SS-DCM) is self assembled by a rationally designed amphiphilic lactose derivative (1), which features a surface lactose corona, a disulfide linkage, and an activatable DCM near-infrared (NIR) probe moiety. Taking advantage of the disulfide linkage, Lac-SS-DCM can be triggered to disassemble by glutathione (GSH) and simultaneously activate the dormant NIR, which allows for a drug-loaded vesicle capable of both therapies in cancer cells where a higher GSH concentration exists and real-time monitoring of drug release. Furthermore, Lac-SS-DCM demonstrates excellent HepG2 target ability as well as higher anticancer efficacy and reduced side effects compared to those of free DOX through lactose-mediated endocytosis resulting from the surface lactose corona, which acts as a multivalent galectin-targeting ligand. As a multifunctional drug delivery compound with perfect synchronization of targeting, imaging, monitoring, and controllable drug release, we believe this activatable glyco-nanovesicle, readily modulated for imaging of different tumors by incorporation of unique targeting entities on the vesicle surface, would be of broad interest for cancer diagnosis and therapy.