[6]-Shogaol/β-CDs inclusion complex: preparation, characterisation, in vivo pharmacokinetics, and in situ intestinal perfusion study

Abstract

Aims: The aim was to improve the absorption and bioavailability of [6]-shogaol with β-cyclodextrin (β-CD) prior to in vitro and in vivo evaluation.

Methods: [6]-Shogaol/β-CDs inclusion complexes (6-S-β-CDs) were developed using saturated aqueous solution method and characterised with appropriate techniques. The absorption and bioavailability potential of [6]-shogaol was evaluated via in vivo pharmacokinetics and in situ intestinal perfusion.

Results: The results of characterisation showed that 6-S-β-CDs (drug loading, 7.15%) were successfully formulated. In vitro release study indicated significantly improved [6]-shogaol release. Pharmacokinetic parameters such as C_max, AUC_0–36 h, and oral relative bioavailability (about 685.36%) were substantially enhanced. The in situ intestinal perfusion study revealed that [6]-shogaol was markedly absorbed via passive diffusion in the intestinal segments, and duodenum followed by ileum and jejunum.

Conclusions: Cyclodextrin inclusion technology could enhance the intestinal absorption and oral bioavailability of hydrophobic drugs like [6]-shogaol.

Keywords:

• [6]-Shogaol
• β-CD
• inclusion complex
• bioavailability
• in situ intestinal perfusion

Acknowledgements

The authors thank the University Ethics Committee for the kind guidance in the animal experiments.

Disclosure statement

The authors report no conflict of interest.

Additional information

Funding

This work was supported by National Natural Science Foundation of China (81473172, 81503025, 81720108030) and National “Twelfth Five-Year” Plan for Science & Technology Support (Grant 2013BAD16B07-1).