Interaction of Antimalarial Agent Artemisinin with Cyclodextrins

To obtain an effective solution of the poorly water soluble antimalarial agent artemisinin, the use of several kinds of cyclodextrins (CDs) as solubilizers was examined. The following CDs were used in this study: α-CD, β-CD, γ-CD as parent CDs, 2-hydroxypropyl-β-CD (HP-β-CD), sulfobutyl ether β-CD (...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2000-01, Vol.26 (6), p.613-619
Main Authors: Usuda, M., Endo, T., Nagase, H., Tomono, K., Ueda, H.
Format: Article
Language:English
Subjects:
Antimalarials - chemistry
Artemisinin
Artemisinins
Chemistry, Pharmaceutical
Cyclodextrins
Cyclodextrins - chemistry
Drug Compounding - methods
Drug Interactions
Drug Stability
Hydrolysis
Polymers - chemistry
Sesquiterpenes - chemistry
Solubility
Solubilization ability
Water - chemistry
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Summary:To obtain an effective solution of the poorly water soluble antimalarial agent artemisinin, the use of several kinds of cyclodextrins (CDs) as solubilizers was examined. The following CDs were used in this study: α-CD, β-CD, γ-CD as parent CDs, 2-hydroxypropyl-β-CD (HP-β-CD), sulfobutyl ether β-CD (SBE7-β-CD), heptakis (2,6-di-O-methyl)-β-CD (DM-β-CD), 2,3,6-partially methylated-β-CD (PM-β-CD) as modified CDs, and glucosyl-β-CD (G1-β-CD), and maltosyl-β-CD (G2-β-CD) as branched CDs. The solubility curves of artemisinin with CDs can all be classified as type AL. The apparent stability constants for artemisinin-parent CD complexes increased in the order of α- < γ- ≤ β-CD. The constants for artemisinin-β-CD derivative (and β-CD) complexes increased in the order of G2-β-CD ≅ G1-β-CD cong; PM-β-CD ≅ β-CD < HP-β-CD < SBE7-β-CD < DM-β-CD. These results suggest that the addition of CDs enables the solubilization of artemisinin.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-100101276