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

Title
2D Inorganic-Antimalarial Drug-Polymer Hybrid with pH-Responsive Solubility
Authors
Kim, Ji-YeongYang, Jae-HunLee, Ji-HeeChoi, GoeunPark, Dae-HwanJo, Mi-ReaChoi, Soo-JinChoy, Jin-Ho
Ewha Authors
최진호양재훈
SCOPUS Author ID
최진호scopus; 양재훈scopus
Issue Date
2015
Journal Title
CHEMISTRY-AN ASIAN JOURNAL
ISSN
1861-4728JCR Link1861-471XJCR Link
Citation
vol. 10, no. 10, pp. 2264 - 2271
Keywords
artesunic acidbioavailabilitylayered compoundspolymerszinc basic salt
Publisher
WILEY-V C H VERLAG GMBH
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
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 EU-DRAGIT 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.
DOI
10.1002/asia.201500347
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자연과학대학 > 화학·나노과학전공 > Journal papers
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