Institute of Chemical and Engineering Sciences, A*STAR (Agency for Science, Technology and Research), 1 Pesek Road, Jurong Island, 627833, Singapore.
Institute of Chemical and Engineering Sciences, A*STAR (Agency for Science, Technology and Research), 1 Pesek Road, Jurong Island, 627833, Singapore.
Colloids Surf B Biointerfaces. 2018 Jan 1;161:83-93. doi: 10.1016/j.colsurfb.2017.10.020. Epub 2017 Oct 7.
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 5min. 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.
通过共喷雾干燥，用转糖基食品添加剂（Hsp-G 和甜菊糖-G）将抗疟药青蒿素（ART）制成无定形固体分散体，改善了其水难溶性的生物制药特性。所制备的 ART/Hsp-G 和 ART/Stevia-G 均表现出优异的溶解性能，药物在 5 分钟内快速释放超过 95%，而未处理的 ART 在 5 分钟内仅溶解 4%。与未处理的 ART 相比，制剂中 ART 的过饱和溶解度提高了 2 倍。储存稳定性测试表明，这些制剂在室温下和低湿度（<18%RH）条件下化学稳定。然而，高湿度（75%RH）会引起再结晶，并导致固体分散体物理外观发生变化。此外，转糖基食品添加剂和 ART 配方样品对 Caco-2 细胞系均表现出低细胞毒性，表明它们具有良好的生物相容性。因此，用转糖基食品添加剂将 ART 制成固体分散体是一种提高水难溶性 ART 生物利用度的潜在安全有效的方法。
