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Dissolution enhancement of artemisinin with β-cyclodextrin
Mitali Kakran1, Nanda Gopal Sahoo, Lin Li
1School of Mechanical and Aerospace Engineering, Nanyang Technological University, Singapore.
Chemical & Pharmaceutical Bulletin
|May 3, 2011
Summary
Fabricating artemisinin (ART) nanoparticles and complexes with beta-cyclodextrin (β-CD) significantly enhanced ART
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Artemisinin (ART) exhibits poor solubility, limiting its therapeutic efficacy.
- Developing strategies to enhance ART dissolution is crucial for improving its bioavailability.
Purpose of the Study:
- To improve the dissolution rate of artemisinin (ART) by fabricating it with beta-cyclodextrin (β-CD).
- To characterize the fabricated ART nanoparticles and ART/β-CD complexes and evaluate their dissolution profiles.
Main Methods:
- Fabrication of ART nanoparticles and ART/β-CD complexes using evaporative precipitation of nanosuspension.
- Characterization using SEM, FT-IR, XRD, and DSC.
- Dissolution testing and statistical analysis of dissolution data.
Main Results:
- Successful fabrication of ART nanoparticles and ART/β-CD complexes.
- Evidence of interaction between ART and β-CD, suggesting complex formation.
- ART/β-CD complexes exhibited significantly faster dissolution rates compared to pure ART.
- Reduced crystallinity and formation of triclinic polymorphic form of free ART in complexes contributed to enhanced dissolution.
Conclusions:
- Evaporative precipitation of nanosuspension is an effective method for fabricating ART nanoparticles and ART/β-CD complexes with improved dissolution.
- The enhanced dissolution is attributed to smaller particle size, inclusion complex formation, polymorphic transformation, and reduced crystallinity.
- This approach offers a promising strategy for enhancing the therapeutic potential of artemisinin.
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