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 (<b>1</b>), 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

One-Step Synthesis of Dual Clickable Nanospheres via Ultrasonic-Assisted Click Polymerization for Biological Applications

Dual clickable nanospheres (DCNSs) were synthesized in one step using an efficient approach of ultrasonic-assisted azide–alkyne click polymerization, avoiding the need of surfactants. This novel approach presents a direct clickable monomer-to-nanosphere synthesis. Field emission scanning electron microscopy (FESEM), Fourier transform infrared spectroscopy (FTIR), and dynamic laser scattering (DLS) were used to characterize the synthesized DCNSs. Numerous terminal alkynyl and azide groups on the surface of DCNSs facilitate effective conjugation of multiple molecules or ligands onto a single nanocarrier platform under mild conditions. To exemplify the potential of DCNSs in biological applications, (1) multivalent glyconanoparticles (GNPs) were prepared by clicking DCNSs with azide-functionalized and alkyne-functionalized lactose sequentially for the determination of carbohydrate-galectin interactions with quartz crystal microbalance (QCM) biosensor. Using protein chip (purified galectin-3 coated on chip) and cell chip (Jurkat cells immobilized on chip), the QCM sensorgrams showed excellent binding activity of GNPs for galectins; (2) fluorescent GNPs were prepared by clicking DCNSs with azide-functionalized Rhodamine B and alkyne-functionalized lactose sequentially in order to target galectin, which is overexpressed on the surface of Jurkat cells. The fluorescent images obtained clearly showed the cellular internalization of fluorescent GNPs. This fluorescent probe could be easily adapted to drugs to construct lectin-targeted drug delivery systems. Thus, DCNSs prepared with our method may provide a wide range of potential applications in glycobiology and biomedicine

Supramolecular Vesicles Based on Complex of Trp-Modified Pillar[5]arene and Galactose Derivative for Synergistic and Targeted Drug Delivery

Supramolecular Vesicles Based on Complex of Trp-Modified Pillar[5]arene and Galactose Derivative for Synergistic and Targeted Drug Deliver