2D Inorganic-Antimalarial Drug-Polymer Hybrid with pH-Responsive Solubility.

Autor: Kim JY; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea., Yang JH; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea., Lee JH; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea., Choi G; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea., Park DH; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea., Jo MR; Department of Food Science and Technology, Seoul Women's University, Seoul, 139-774, South Korea., Choi SJ; Department of Food Science and Technology, Seoul Women's University, Seoul, 139-774, South Korea., Choy JH; Center for Intelligent Nano-Bio Materials (CINBM), Department of Chemistry and Nano Science, Ewha Womans University, Seoul, 120-750, South Korea. jhchoy@ewha.ac.kr.
Jazyk: angličtina
Zdroj: Chemistry, an Asian journal [Chem Asian J] 2015 Oct; Vol. 10 (10), pp. 2264-71. Date of Electronic Publication: 2015 Jun 17.
DOI: 10.1002/asia.201500347
Abstrakt: Artesunic acid (ASH), an antimalarial drug, has low oral bioavailability due to its low aqueous solubility. To overcome this problem, artesunate (AS) was intercalated into zinc basic salt (ZBS) via co-precipitation. AS was immobilized with a tilted double layer arrangement, which was also confirmed by XRD and 1-D electron density mapping. In order to decrease the release rate of AS under gastrointestinal conditions and to simultaneously increase the release rate of AS under intestinal conditions, ZBS-AS was coated with EUDRAGIT L100 (ZBS-AS-L100). Finally, we performed an in-vivo pharmacokinetic study to compare the oral bioavailability of AS of ZBS-AS-L100 with that of ASH. Surprisingly, it was found that the former is 5.5 times greater than the latter due to an enhanced solubility of AS thanks to the ternary hybridization with ZBS and EUDRAGIT L100. Therefore, the present ZBS-AS-L100 system has a great potential as a novel antimalarial drug formulation with pH selectivity and enhanced bioavailability.
(© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
Databáze: MEDLINE
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