A novel host-guest complex based on biotin functionalized polyamine-β-cyclodextrin for tumor targeted delivery of luteolin

Abstract Luteolin (LU) shows significant bioactivities, but inherent poor aqueous solubility and stability severely hamper its applications in pharmaceutical application. Herein, a series of efficient tumor targeted drug carriers were designed and synthesised by binding biotin to a β-cyclodextrin through a polyamine chain. Their characteristics and inclusion behavior with LU in aqueous and solid states were investigated by UV-Vis, NMR, XRD, FT-IR, TG, and SEM. Moreover, tumor targeted effect of inclusion complexes was confirmed by the Confocal Laser Scanning Microscopy (CLSM) images and the decrease of anti-cancer ability owing to biotin receptor saturated with excess biotin added. Besides, anticancer activity and solubility of inclusion complexes were greatly improved by 27 and 1423 folds, respectively, compared with free LU. It suggests biotin-polyamine-β-CDs (BCDs) might be promising tumor targeted carriers, which are expected to be applied in the pharmaceutical field for further research.