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AAPS PharmSciTech

, 20:244 | Cite as

Effects of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Inclusions on the Degradation of Magnolol by Intestinal Bacteria

  • Lan Tang
  • Zhuanfeng Zhu
  • Miao Xie
  • Lipeng Cao
  • Xiao Lan Yu
  • Ran Zhang
  • Zhimin Ou
  • Weiguang ShanEmail author
  • Zhenhai ZhangEmail author
Research Article
  • 49 Downloads

Abstract

Cyclodextrin (CD) inclusions are generally used to increase the solubility of poorly soluble drugs. In this study, magnolol (MAG) was used as a model drug for exploring the effects of CD on the degradation of pharmaceutical drugs by intestinal microflora. MAG/β-cyclodextrin (β-CD) and MAG/hydroxypropyl-β-CD (HP-β-CD) inclusion complexes were successfully prepared by the saturated aqueous solution and freeze-drying methods, respectively. Structural characterisation along with analyses of solubility, residual water content and drug content of the inclusion complexes was performed. The intestinal microflora of male rats was used to study MAG degradation in vitro. At three concentrations, the degradation of both the inclusion complexes was slower than that of the MAG monomer, MAG and CD mixtures and the MAG-poloxamer 188 micelle. There were no statistically significant differences in the degradation of the MAG/β-CD and MAG/HP-β-CD inclusion complexes. A simulation first-order equation of the degradation parameters revealed that the degradation of the inclusion complexes was slower and pronounced, judging by slope. The experimental findings were verified by molecular docking for predicting the stable molecular structure of the inclusion complexes. In conclusion, the inclusion complexes partially protected MAG from degradation by the intestinal bacteria.

KEY WORDS

intestinal flora magnolol inclusion complex degradation 

Abbreviations

CD

Cyclodextrin (Fw=~1135, purity ≧98%)

MAG

Magnolol

MAG/β-CD

MAG/β-cyclodextrin

MAG/HP-β-CD

MAG/hydroxypropyl-β-cyclodextrin (DS = 6.1, Fw = 1489, purity ≥ 91%)

RSD

Relative standard deviation

Notes

Compliance with Ethical Standards

The Laboratory Animal Welfare Ethics Committee of Zhejiang University of Technology approved the animal experiments.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Lan Tang
    • 1
  • Zhuanfeng Zhu
    • 1
  • Miao Xie
    • 1
  • Lipeng Cao
    • 1
  • Xiao Lan Yu
    • 1
  • Ran Zhang
    • 1
  • Zhimin Ou
    • 1
  • Weiguang Shan
    • 1
    Email author
  • Zhenhai Zhang
    • 2
    • 3
    Email author
  1. 1.College of Pharmaceutical ScienceZhejiang University of TechnologyHangzhouPeople’s Republic of China
  2. 2.Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese MedicineNanjingPeople’s Republic of China
  3. 3.Jiangsu Province Academy of Traditional Chinese MedicineNanjingPeople’s Republic of China

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