13-cyclodextrin-based nanosponges for crocetin delivery: Physicochemical characterization, aqueous solubility, and bioactivity

Crocetin (CRT) is a natural carotenoid compound with promising health benefits but its use is restricted because of the poor aqueous solubility. Therefore, cyclodextrin-based nanosponges (CDNSs), a kind of water-soluble supramolecular macrocyclic polymer, was employed to load CRT for improving the solubility. The 13-CDNSs with different molar ratio of 13-CD and crosslinker were synthesized and 13-CDNS 1:8 was chosen. The loading capacity (LC) and complexation efficiency (CE) of prepared CRT-loaded 13-CDNS were about 17.92% and 94.64%. The formation of inclusion and non-inclusion structure of CRT-loaded 13-CDNS was confirmed by different techniques. The surface properties and dispersibility were also studied. Besides, the water solubility of CRT was significantly increased to 7.27 & mu;g/mL. The antioxidant activity of CRT was enhanced. The in vitro cytotoxicity of CRT for normal cells was reduced and for tumor cells was increased through the loading of 13-CDNS. In summary, this work demonstrated 13-CDNS could be used for the delivery of CRT and promote the application of CRT in many fields.