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

    Year: 2018

    Journal: Colloid Surf. B-Biointerfaces, Volume 161, JAN 1, page 83–93

    Authors: Letchmanan, Kumaran; Shen, Shou-Cang; Ng, Wai Kiong; Tan, Reginald S. H.

    Organizations: GlaxoSmithKline (GSK) [R-279-000-329592]; Science and Engineering Research Council of A*STAR (Agency for Science, Technology and Research), Singapore; National University of Singapore

    Keywords: Cytotoxicity; Physicochemical stability; Drug delivery; Functionalized food additives; Supersaturation solubility

    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. (C) 2017 Elsevier B.V. All rights reserved.
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