Li Yan, Zheng Jinkai, Xiao Hang, McClements David Julian
Biopolymers and Colloids Research Laboratory, Department of Food Science, University of Massachusetts, Amherst, Massachusetts 01003.
Food Hydrocoll. 2012 Jun 1;27(2):517-528. doi: 10.1016/j.foodhyd.2011.08.017. Epub 2011 Sep 17.
Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.
从柑橘皮中提取的多甲氧基黄酮（PMFs）具有强大的抗癌活性，但它们是高度疏水的分子，在环境温度和体温下在水和油中的溶解度都很差，这限制了它们的生物利用度。研究了将PMFs包裹在基于纳米乳液的递送系统中以促进其在营养保健品和药品中应用的可能性。考察了油相类型（玉米油、中链甘油三酯、橙油）、乳化剂类型（β-乳球蛋白、溶血卵磷脂、吐温、十二烷基三甲基溴化铵）和中性助溶剂（甘油和乙醇）对负载PMF的纳米乳液形成和稳定性的影响。除了十二烷基三甲基溴化铵外，使用高压均质法可以为所有类型的乳化剂形成纳米乳液（r < 100 nm）。通过改变乳化剂类型，脂质滴电荷可以从高度阳离子型（十二烷基三甲基溴化铵）变为接近中性（吐温），再变为高度阴离子型（β-乳球蛋白、溶血卵磷脂）。制备后所有纳米乳液中都形成了PMF晶体，这些晶体在储存期间有沉淀的趋势。PMF晶体的尺寸、形态和聚集情况取决于制备方法、乳化剂类型、油相类型和助溶剂的添加。这些结果对于开发在应用温度下油溶性和水溶性都很差的生物活性成分递送系统具有重要意义。
