Enhanced Bioavailability of Curcumin Nanoemulsions Stabilized with Phosphatidylcholine Modified with Medium Chain Fatty Acids.
Enhanced Bioavailability of Curcumin Nanoemulsions Stabilized with Phosphatidylcholine Modified with Medium Chain Fatty Acids.
复制标题
用中链脂肪酸修饰的磷脂酰胆碱稳定姜黄素纳米乳液，增强其生物利用度。
DOI：
10.2174/1567201813666160919142811
复制
发表时间：
2017
影响因子：
2.4
通讯作者：
H. García
中科院分区：
文献类型：
--
作者：
A. A. Ochoa;J. A. Hernández;A. Cavazos;Ida Soto;M. Sánchez;E. J. Vernon‐Carter;H. García
背景
姜黄素是一种天然的油溶性多酚化合物，具有强效的抗癌、抗炎和抗氧化活性。在其游离形式下，由于其非常低的溶解度，它在肠道中的吸收非常差。利用纳米乳作为载体是提高姜黄素生物利用度的可行途径。为此，用于稳定纳米乳液的乳化剂的选择对于实现所需的功能是最重要的。
方法
磷脂酰胆碱（PC）和富含中链脂肪酸（42.5mol%）的磷脂酰胆碱（PCE）与作为助表面活性剂的甘油组合，用于制备分别编码为NEPC和NEPCE的水包油纳米乳液。
结果
与NEPC相比，NEPCE显示出显著更小的平均液滴尺寸（30 nm）、相等的包封率（100%）、更好的液滴稳定性，并且在储存时间（120天，4ºC）期间遭受更低的包封率损失（3%）。生物利用度，姜黄素浓度与时间的曲线下的面积，最大姜黄素血浆浓度，测量，是在一般情况下显着高于NEPCE比NEPC，姜黄素粗水悬浮液（CCS）。此外，NEPCE在肝脏和肺中产生的姜黄素浓度显著高于NEPC和CCS。
结论
这些数据支持富含中链脂肪酸的磷脂酰胆碱在增加用于治疗应用的纳米乳剂的生物利用度方面的作用。
BACKGROUND
Curcumin is a natural, oil-soluble polyphenolic compound with potent anticancer, anti-inflammatory, and antioxidant activities. In its free form, it is very poorly absorbed in the gut due to its very low solubility. The use of nanoemulsions as carrier is a feasible way for improving curcumin bioavailability. To this end, the choice of emulsifying agent for stabilizing the nanoemulsions is of the upmost importance for achieving a desired functionality.
METHODS
Phosphatidylcholine (PC) and phosphatidycholine enriched (PCE) with medium chain fatty acids (42.5 mol %) in combination with glycerol as co-surfactant, were used for preparing oil-in water nanoemulsions coded as NEPC and NEPCE, respectively.
RESULTS
NEPCE displayed significantly smaller mean droplet size (30 nm), equal entrapment efficiency (100%), better droplet stability and suffered lower encapsulation efficiency loss (3%) during storage time (120 days, 4ºC) than NEPC. Bioavailability, measured in terms of area under the curve of curcumin concentration versus time, and maximum curcumin plasma concentration, was in general terms significantly higher for NEPCE than for NEPC, and for curcumin coarse aqueous suspension (CCS). Also, NEPCE produced significantly higher curcumin concentrations in liver and lung than NEPC and CCS.
CONCLUSION
These data support the role of phosphatidylcholine enriched with medium chain fatty acids to increase the bioavailability of nanoemulsions for therapeutic applications.