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

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 tec...

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Bibliographic Details
Published in:Journal of microencapsulation 2019-07, Vol.36 (5), p.500-512
Main Authors: Li, Ran, Bao, Rui, Yang, Qiu-Xuan, Wang, Qi-Long, Adu-Frimpong, Michael, Wei, Qiu-Yu, Elmurat, Toreniyazov, Ji, Hao, Yu, Jiang-Nan, Xu, Xi-Ming
Format: Article
Language:English
Subjects:
Animals
beta-Cyclodextrins - chemistry
bioavailability
Biological Availability
Catechols - administration & dosage
Catechols - pharmacokinetics
Drug Carriers - chemistry
in situ intestinal perfusion
inclusion complex
Intestinal Absorption
Intestinal Mucosa - metabolism
Male
Rats, Sprague-Dawley
Shogaol
Zingiber officinale - chemistry
β-CD
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Summary: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.
ISSN:0265-2048
1464-5246
DOI:10.1080/02652048.2019.1649480