Abstract
Although β-cyclodextrin (β-CD) inclusion is known to improves the stability and solubility of trans-cinnamaldehyde (CA), but data on the in vitrorelease, pharmacokinetics, and pharmacodynamics of such inclusion complexes are lacking. In this study, an inclusion complex of CA and β-CD (CA-β-CD) inclusion complex was prepared using a saturated solution method.Its in vitro release was determined using the dialysis bag method with a molecular cut-off of 1000 D, while its in vivo pharmacokinetics were studied in a rat model. A carrageenan-induced acute inflammation mouse model of foot swelling was used to evaluate the effects of the inclusion complex on drug efficacy. The CA-β-CD inclusion complex had a lower release rate within 2 h and a higher release rate than CA after 2 h in both release media. In vivopharmacokinetic studies of the CA-β-CD inclusion showed a decrease in peak concentration, a significant increase in half-life (p<0.05), and an increase in bioavailability. A pharmacodynamic study on the effects of the inclusion complex on toe swelling in mice showed that it had slightly slower effects than the CA, but a relatively long-lasting swelling inhibition effect. The above findings suggest that CA has a certain slow-release behavior in vitro and in vivo after being encapsulated by β-CD, which has an effect on the drug’s efficacy.