Novel artemisinin and curcumin micellar formulations: Drug solubility studies by NMR spectroscopy
✍ Scribed by Silvia Lapenna; Anna Rita Bilia; Gareth A. Morris; Mathias Nilsson
- Book ID
- 102396595
- Publisher
- John Wiley and Sons
- Year
- 2009
- Tongue
- English
- Weight
- 173 KB
- Volume
- 98
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
Artemisinin, a potent antimalarial drug derived from Artemisia annua L., and curcumin, a polyphenol extracted from the roots of Curcuma longa L., are reported to exert a synergistic antimalarial action, albeit manifesting a low bioavailability. In fact, both these molecules are poorly soluble in aqueous environments. In this study, we report a DOSY investigation of the solubilisation capacity of micelles of sodium dodecyl sulphate (SDS) for artemisinin and curcumin, individually and in combination. The aqueous solubility of artemisinin was enhanced approximately 25-fold by 40 mM SDS, and 50-fold by 81 mM SDS, while that of curcumin was increased to 2 mM by 81 mM SDS. In addition, we performed model studies on the use of the surface-active radical scavenger octanoyl-6-O-ascorbic acid (ASC8) to combine solubilisation with protection against oxidation for the chemically labile artemisinin. A 16-fold enhancement of artemisinin solubility was measured in a solution containing 40 mM SDS and 60 mM ASC8. Even after treatment with 60 mM hydrogen peroxide, more than a 30-fold excess, almost half the artemisinin remained, suggesting a potentially useful combination of the surface activity and antioxidant properties of the novel binary SDS:ASC8 system.