To prepare ecdysterone (ES)/hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex, thus improving the water solubility and bioavailability of ES. Phase-solubility study was performed to study the mass ratio of ES and HP-β-CD. Then, the ES/HP-β-CD inclusion complex was prepared by the solvent evaporation method, and its physicochemical properties were characterised using the SEM, DSC, XRD, 1HNMR and FT-IR. In addition, in vitro dissolution and bioavailability (oral and transdermal) experiments were also conducted. The inclusion complex was formed with ES and HP-β-CD at the mass ratio of 1:1. ES existed in an amorphous form in the inclusion complex. The equilibrium solubility of ES/HP-β-CD inclusion complex in SGF (simulated gastric fluid) and SIF (simulated intestinal fluid) was 50.6 ± 0.11 mg/mL and 75.9 ± 0.38 mg/mL in SGF and SIF, which was 5.93 and 9.96 times higher than that of free ES, respectively. The ES/HP-β-CD inclusion complex had better dissolution ability and transdermal permeability than the free ES. The oral bioavailability and the transdermal bioavailability were respectively increased by 2.97 times and 1.92 times compared with the free ES. These data suggest that the ES/HP-β-CD inclusion complex can be developed as potential pharmaceutical product for future clinical applications.
Keywords: Ecdysterone; HP-β-CD; bioavailability; inclusion complex.