Abstract: The aim of the present st

Abstract: The aim of the present study is to develop and optimize self-nanoemulsifying drug delivery systems (SNEDDS) to improve the per-oral bioavailability of poorly soluble herb active ingredient, Dihydromyricetin (DMY), and to evaluate its characterization and in vitro performance. Solubility of DMY was estimated in various vehicles to select proper components combinations. MCT(oil), Cremophor-RH40 or Tween-80 (surfactants) as well as glycerol (co-surfactants) were employed to construct pseudo-ternary phase diagrams. Combine with characterization, emulsification grade, thermodynamic stability and robustness to dilution tests were selected most optimize formulations. Formulations composed of MCT: Cremophor-RH40: glycerol = 9:14:7 was selected. The partical sizes of the DMY-SNEDDS (O/W) was 56.54±0.36 nm, zeta-Potential was -5.21±0.54 mV, PDI value was 0.312±0.08, the drug loading was 45mg/kg. The in vitro release profile of DMY-SNEDDS was found significant in comparison to the plain DMY suspension. These results demonstrate the potential use of SNEDDS for improving the bioavailability of poor water soluble compounds, such as DMY.
Keywords: Dihydromyricetin; self-nanoemulsifying drug delivery systems; bioavailability; characterization; drug release

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结果 (简体中文) 1: [复制]

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Abstract: The aim of the present study is to develop and optimize self-nanoemulsifying drug delivery systems (SNEDDS) to improve the per-oral bioavailability of poorly soluble herb active ingredient, Dihydromyricetin (DMY), and to evaluate its characterization and in vitro performance. Solubility of DMY was estimated in various vehicles to select proper components combinations. MCT(oil), Cremophor-RH40 or Tween-80 (surfactants) as well as glycerol (co-surfactants) were employed to construct pseudo-ternary phase diagrams. Combine with characterization, emulsification grade, thermodynamic stability and robustness to dilution tests were selected most optimize formulations. Formulations composed of MCT: Cremophor-RH40: glycerol = 9:14:7 was selected. The partical sizes of the DMY-SNEDDS (O/W) was 56.54±0.36 nm, zeta-Potential was -5.21±0.54 mV, PDI value was 0.312±0.08, the drug loading was 45mg/kg. The in vitro release profile of DMY-SNEDDS was found significant in comparison to the plain DMY suspension. These results demonstrate the potential use of SNEDDS for improving the bioavailability of poor water soluble compounds, such as DMY.<br>关键词：二氢杨梅素; 自纳米乳化药物传递系统; 生物利用度; 表征; 药物释放

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结果 (简体中文) 2:[复制]

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摘要：本研究的目的是开发和优化自纳米乳化药物输送系统（SNEDDS），以提高低溶性草本活性成分二氢甲酸酯（DMY）的每次口服生物利用度，并评估其表征和体外性能。DMY 的溶解度被估算在各种车辆中，以选择适当的部件组合。MCT（油）、克里莫莫霍-RH40或Tween-80（表面活性剂）以及甘油（共表面活性剂）被用来构造伪三元相图。结合表征，乳化等级，热力学稳定性和鲁棒性稀释试验选择最优化的配方。由 MCT 组成的配方：克雷莫莫-RH40：甘油 = 9：14：7 被选中。DMY-SNEDDS （O/W）的分段尺寸为 56.54±0.36 nm，Zeta-电位为 -5.21±0.54 mV，PDI值为 0.312±0.08，药物载量为 45mg/kg。与普通DMY悬浮液相比，DMY-SNEDDS的体外释放配置文件显著。这些结果表明，SNEDDS有可能用于提高劣质水溶性化合物（如DMY）的生物利用度。<br>关键词：二氢甲酸;自纳米乳化药物输送系统;生物利用度;特征特征;药物释放

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结果 (简体中文) 3:[复制]

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文摘：为了提高难溶性中草药活性成分二氢杨梅素（dmy）的口服生物利用度，研究和优化自纳米乳化给药系统（snedds），并对其进行表征和体外性能评价。为了选择合适的组分组合，对dmy在不同载体中的溶解度进行了测定。采用mct（油）、cremophor-rh40或tween-80（表面活性剂）和甘油（共表面活性剂）构建拟三元相图。结合表征、乳化度、热力学稳定性和对稀释试验的鲁棒性，筛选出最佳配方。选择由mct:cremophor-rh40:glycerol=9:14:7组成的制剂。dmy-snedds的粒径为56.54±0.36nm，zeta电位为-5.21±0.54mv，pdi值为0.312±0.08，载药量为45mg/kg。与普通DME悬浮液相比，DY-SUNDDS的体外释放曲线显著。这些结果表明，snedds在改善dmy等水溶性差的化合物的生物利用度方面具有潜在的应用前景。<br>关键词：二氢杨梅素；自纳米乳化给药系统；生物利用度；表征；药物释放<br>

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