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.

Automated summary

This study demonstrates the use of cyclodextrin-based nanosponges (CDNSs) as a delivery system for Crocetin (CRT), an otherwise poorly soluble compound with promising health benefits. The inclusion and non-inclusion structures of CRT-loaded 13-CDNS were confirmed, and the water solubility of CRT was significantly increased. The antioxidant activity of CRT was enhanced and its cytotoxicity on normal cells was reduced while increased for tumor cells through the loading of 13-CDNS.