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Supramolecular construction of a targeted and stimuli-responsive drug delivery system is still a challenging task. Herein, GSH-responsive supramolecular prodrug nanoparticles were constructed by the host–guest complexation between a β-d-galactose-functionalized water-soluble pillar[5]arene (GalP5) and a disulfide bond containing camptothecin prodrug (G). The obtained prodrug nanoparticles were stable under physiological conditions, whereas efficient drug release was triggered in a simulated tumor environment with high GSH concentration. In vitro studies revealed that these prodrug nanoparticles preferentially entered asialoglycoprotein receptor-overexpressing HepG2 cells due to the active targeting effect of galactose units. This active targeting effect resulted in the maximization of anticancer efficacy and reduction of the undesirable side effects to normal cells. [ABSTRACT FROM AUTHOR]

The stimuli-responsive behavior of supramolecular nanocarriers is crucial for their potential applications as smart drug delivery systems. We hereby constructed a glucose-responsive supramolecular drug delivery system based on the host-guest interaction between a water-soluble pillar[5]arene ( WP5) and a pyridylboronic acid derivative ( G) for insulin delivery and controlled release under physiological conditions. The approach represents the ideal treatment of diabetes mellitus. The drug loading and in vitro drug release experiments demonstrated that large molecular weight insulin could be encapsulated into the vesicles with high loading efficiency, which, to our knowledge, is the first example of small-size supramolecular vesicles with excellent encapsulation capacity of a large protein molecule. Moreover, FITC-labeled insulin was used to evaluate the release behavior of insulin, and it was demonstrated that high glucose concentration could facilitate the quick release of insulin, suggesting a smart drug delivery system for potential application in controlled insulin release only under hyperglycemic conditions. Finally, we demonstrated that these supramolecular nanocarriers have good cytocompatibility, which is essential for their further biomedical applications. The present study provides a novel strategy for the construction of glucose-responsive smart supramolecular drug delivery systems, which has potential applications for the treatment of diabetes mellitus. [ABSTRACT FROM AUTHOR]

A bola-type supra-amphiphile assembled from a water-soluble pillar[5]arene host (WP5) and a rod-coil guest molecule (G) containing a photoactive 9,10-dialkoxyanthracene group was successfully constructed, which could further assemble into a monolayer supramolecular vesicle. Interestingly, the photodecomposition rate of G was remarkably promoted after its aggregation with WP5, accompanied by the disassembly of the formed supramolecular vesicle, especially with the coassembly of a photosensitizer eosin Y, which has potential applications in phototherapy. [ABSTRACT FROM AUTHOR]

A dual-responsivesupramolecular network based on pillar[6]arene–ferroceniumredox-controllable recognition motifs in polymeric backbones is constructedwith a ferrocenium-functionalized copolymer and a pillar[6]arene copolymer,in which the first example of pillar[6]arene-functionalized copolymerwas synthesized through the reversible addition/fragmentation chain-transfercopolymerization of an acrylate-functionalized pillar[6]arene andmethyl acrylate. The resulting supramolecular network exhibits dramaticallyincreased viscosity than the non-cross-linked mixtures and demonstratesa gel-like behavior on macroscale with a transient-network behaviorrevealed by rheology study. Furthermore, the viscoelastic propertiesof such supramolecular network can be easily controlled by differentexternal stimuli including redox stimulus and competing host/guestreagents. [ABSTRACT FROM AUTHOR]