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  • 02월 26일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제115회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Artesunate-layered zinc hydroxide nanohybrid with enhanced oral bioavailability

2015년 2월 26일 16시 24분 46초
MAT.P-1183 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 15일 (수요일) 16:00~19:00
저자 및
김지영, 양재훈, 최진호*
이화여자대학교 화학.나노과학과, Korea
Low bioavailability of artesunate (AS), anti-malaria drug, is attributed to its low solubility in water. In order to overcome this problem, the novel drug delivery vehicle system with sustained release property was successfully demonstrated by intercalating AS into layered zinc hydroxides (ZBS) via co-precipitation. According to the powder x-ray diffraction analysis, the basal spacing of AS-ZBS nanohybrid was determined to be 2.88 nm, indicating that AS was successfully incorporated into the ZBS layers, which was also confirmed by 1-D electron density mapping analysis and TEM analysis. The fourier transformed infrared spectra revealed that AS molecules were deprotonated and electrostatically incorporated between cationic zinc hydroxide layers without any structural change. Through CHNS analysis, TG analysis and HPLC analysis, the contents of AS for AS-ZBS nanohybrid was determined to be 45.8 wt%. Furthermore, AS-ZBS nanohybrid was coated with Eudragit- L100 (anionic polymer) for the pH-dependent dissolution property (AS-ZBS-L100). AS-ZBS-L100 nanohybrid showed the greatly enhanced dissolution rate of AS in simulated intestinal condition (pH 6.8) compared with the intact AS. In vivo pharmacokinetic study was performed in rats via oral administration to compare the absorption of artesunate for AS-ZBS-L100 nanohybrid and intact AS. According to the plasma concentration-time curve, the pharmacokinetic data such as AUC and Cmax values for the AS-ZBS-L100 nanohybrid (AUC = 177.2 ± 30.1 h mg/L and Cmax = 51.1 ± 14.8 μg/mL) were remarkably larger than those of intact AS (AUC = 23.3 ± 3.4 h mg/L and Cmax = 20.1 ± 4.3 μg/mL). Therefore, AS-ZBS-L100 nanohybrid system has a great potential as a malaria drug formulation with enhanced bioavailability.