Application of transglycosylated stevia and hesperidin as drug carriers to enhance biopharmaceutical properties of poorly-soluble artemisinin

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Application of transglycosylated stevia and hesperidin as drug carriers to enhance biopharmaceutical properties of poorly-soluble artemisinin
Title:
Application of transglycosylated stevia and hesperidin as drug carriers to enhance biopharmaceutical properties of poorly-soluble artemisinin
Journal Title:
Colloids and Surfaces B: Biointerfaces
Keywords:
Publication Date:
07 October 2017
Citation:
Letchmanan, K.; Shen, S. C.; Ng, W. K.; Tan, R. B. H., Application of transglycosylated stevia and hesperidin as drug carriers to enhance biopharmaceutical properties of poorly-soluble artemisinin. Colloids and Surfaces B: Biointerfaces 2018, 161 (Supplement C), 83-93.
Abstract:
Biopharmaceutical properties of poorly water-soluble antimalarial drug, Artemisinin (ART), were improved by formulating amorphous solid dispersions with transglycosylated food additives (Hsp-G and Stevia-G) via co-spray drying. Both the formulated ART/Hsp-G and ART/Stevia-G showed superior dissolution properties with a burst release of more than 95% of drug within 5 min, whereas untreated ART dissolved only 4% in 5 min. The supersaturation solubility of the formulated ART was enhanced by 2-fold as compared with untreated counterpart. The storage stability tests indicated that these formulations chemically stable at room temperature and under low humidity ( < 18% RH) conditions. However, high humidity (75% RH) induced re-crystallization and caused changes in the physical appearance of the solid dispersions. In addition, both the food additives and ART formulated samples showed low cytotoxicity to Caco-2 cell line suggesting their good biocompatibility. Thus, the formation of solid dispersions of ART with transglycosylated food additives is a potentially safe and effective approach to enhance the bioavailability of poorly water-soluble ART.
License type:
http://creativecommons.org/licenses/by-nc-nd/4.0/
Funding Info:
This work was funded by project grant R-279-000-329592 from GlaxoSmithKline (GSK) and the Science and Engineering Research Council of A*STAR (Agency for Science, Technology and Research), Singapore.
Description:
ISSN:
0927-7765
1873-4367
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