以棕榈油为原料制备姜黄素微乳的工艺优化

Ghanesh Muniandy, Chong Shu Xian
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引用次数: 0

摘要

姜黄素是一种天然疏水性多酚,来源于姜黄中的姜黄素类物质。姜黄素通常被称为姜黄,它表现出抗癌、抗炎和抗氧化等巨大的药理作用,因此引起了科学和临床研究人员的兴趣。尽管如此,姜黄素由于其水溶性差和口服生物利用度低,仍然不是临床上批准的药物。因此,采用自微乳给药系统(SMEDDS)来提高姜黄素的溶解度和生物利用度。使用表面活性剂(Tween 80)、共表面活性剂、脂质相(棕榈油)和水相(水)在预配制阶段设计微乳液。使用三元相图来识别制剂中的自微乳液区域。发现这些制剂中的五种(F1、F2、F4、F7和F10)是稳定的,在过夜储存时没有观察到相分离。所有五种制剂(F4除外)都具有较高的透光率(86%–100%),这表明当它们被水以1:100的比例稀释时,形成了稳定的微乳液。将姜黄素负载到F1、F2、F7和F10中制备姜黄素微乳。只有F1和F2姜黄素微乳液表现出清晰的外观,然而,F7和F10形成混浊的溶液,这表明乳液的形成。结果表明,表面活性剂/助表面活性剂与油的比例为9:1的F1和F2最适合配制姜黄素微乳。
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Optimisation of Curcumin Microemulsions Using Palm Oil
Curcumin is a natural hydrophobic polyphenol derived from the curcuminoids of Curcuma longa. Curcumin is commonly known as turmeric and it gains the interest of scientific and clinical researchers as it exhibits great pharmacological benefits such as anti-cancer, antiinflammatory and anti-oxidant properties. Nevertheless, curcumin is still not an approved drug in clinical settings due to its poor aqueous solubility and low oral bioavailability. Therefore, a self-microemulsifying drug delivery system (SMEDDS) was used as an approach to enhance the solubility and bioavailability of curcumin. The microemulsion was devised in a pre-formulation phase using a surfactant (Tween 80), a co-surfactant (polyethylene glycol, PEG 400), a lipid phase (palm oil) and an aqueous phase (water). A ternary phase diagram was used to identify the self-microemulsifying region in a formulation. Five of these formulations (F1, F2, F4, F7 and F10) were found to be stable with no phase separation observed upon overnight storage. All of the five formulations (except F4) possessed a high percentage of transmittance (86%–100%), which signified the formation of a stable microemulsion when they were diluted in a 1:100 ratio by water. Curcumin microemulsions were formulated by loading curcumin into F1, F2, F7 and F10. Only F1 and F2 curcumin microemulsions exhibit a clear appearance, however, F7 and F10 form a turbid solution, which indicates the formation of the emulsion. The results indicated that F1 and F2 which contain a high surfactant/co-surfactant-to-oil ratio of 9:1 is optimum to formulate the curcumin microemulsions.
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