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Increased stability and solubility of dihydroartemisinin in aqueous solution through the formation of complexes with 2-hydroxypropyl-β-cyclodextrin

Xiao-Yun Zhang, Jian-Ping Liu*, Hua Qiao, Kui-Yuan Huang, Yan-Bin Shi, Shu-Mei Song, Jing-Man Ni   

  1. 1. College of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
    2. College of Pharmacy, Lanzhou University, Gansu 730000, China
    3. Department of Pharmaceutics, the First Hospital of Lanzhou University, Gansu 730000, China
  • Received:2009-03-25 Revised:2009-05-10 Online:2009-06-15 Published:2009-06-15
  • Contact: Jian-Ping Liu*

Abstract:

The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) on the solubility of dihydroartemisinin (DHA) in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β-cyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ºC was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin.

Key words: Dihydroartemisinin, Dihydroartemisinin, 2-Hydroxypropyl-β-cyclodextrin, 2-Hydroxypropyl-β-cyclodextrin, Solubility, Solubility, Stability, Stability

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