Conjugating aldoxorubicin to supramolecular organic frameworks: polymeric prodrugs with enhanced therapeutic efficacy and safety

Abstract

Phase I-III clinical studies show that aldoxorubicin (AlDox), a prodrug of doxorubicin (Dox), displays superior cardiotocity over Dox, but does not demonstrate a survival benefit in the entire patients. Here...

Supramolecular Organic Frameworks: Exploring Water-Soluble, Regular Nanopores for Biomedical Applications

“…The tetrahedral backbone can be modified by introducing different substituents to afford T1b-h , which coassembled with CB[8] to give rise to similar supramolecular architectures dSOF1b – h (Scheme ). ,,− dSOF1g and dSOF1h formed by T1g or T1h displayed the highest water solubility of 8.0 mM, indicating that their hydrophilic groups could remarkably increase the water solubility of the frameworks. The maximum tolerated doses (MTDs) of Wistar rats for dSOF1a , dSOF1b , dSOF1g , and dSOF1h (three males and three females per group) were determined to be 17, 31, 49, and 77 mg/kg, respectively, which corresponded to values of 0.16, 0.30, 0.47, and 0.74 g for an adult of 60 kg weight by assuming a conversion coefficient of 6.25.…”

“…Their homogeneity enabled the inclusion process to take place very rapidly because all of the experiments related to this process were time-independent. dSOF1a – h were prepared in boiling water at the highest concentration of the tetrahedral components ,,− ,− but could maintain their nanoscale sizes at the low concentration of 50 μM at room temperature, indicating that the peripheral substituents of the tetrahedral components did not affect the stability of the frameworks. Therefore, they could not only function as antidotes to neutralize the anticoagulation activity of residual heparins and alleviate the posttreatment phototoxicity of residual PDAs but also work well as nonequilibrium carriers, conducting in situ loading and the intracellular delivery of antitumor drugs and PDAs, ,,,, which has been ascribed to the so-called enhanced permeability and retention (EPR) effect .…”

“…Therefore, they could not only function as antidotes to neutralize the anticoagulation activity of residual heparins and alleviate the posttreatment phototoxicity of residual PDAs but also work well as nonequilibrium carriers, conducting in situ loading and the intracellular delivery of antitumor drugs and PDAs, ,,,, which has been ascribed to the so-called enhanced permeability and retention (EPR) effect . Apart from inclusion-based biomedical applications, dSOFs can also be conjugated with antitumor agents, forming new supramolecular prodrugs to attain enhanced efficacy . This Account highlights the advances.…”

“…33 Apart from inclusion-based biomedical applications, dSOFs can also be conjugated with antitumor agents, forming new supramolecular prodrugs to attain enhanced efficacy. 26 This Account highlights the advances.…”

Pyrrole/thiophene π‐bridged two triphenylamine electron donor and substituted thiobarbituric electron acceptor for D‐π‐A‐D‐featured DSSC applications

“…The coupling of carbazole and coumarin units enhanced the PCE to 5.53% than the pristine coumarin. [ 13 ] The synergism between phenothiazine and dithiafulvenyl unit enhanced PCE from 4.16 to 5.87%. [ 14 ] Two donor molecules such as triphenylamine and coumarin were corroborated and designed D‐D‐π‐A photosensitizers to enhance light absorption and optical properties (PCE = 4.99%).…”