Ochoa-Flores Angélica A, Hernández-Becerra Josafat A, Cavazos-Garduño Adriana, Soto-Rodríguez Ida, Sanchez-Otero Maria Guadalupe, Vernon-Carter Eduardo J, García Hugo S
UNIDA, Instituto Tecnológico de Veracruz, M.A. de Quevedo 2779, Col. Formando Hogar, Veracruz, Ver. 91897, Mexico.
Facultad de Bioanalisis, Universidad Veracruzana, Carmen Serdan S/N, Veracruz, Ver. 91700, Mexico.
Curr Drug Deliv. 2017;14(3):377-385. doi: 10.2174/1567201813666160919142811.
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.
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.
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.
These data support the role of phosphatidylcholine enriched with medium chain fatty acids to increase the bioavailability of nanoemulsions for therapeutic applications.
姜黄素是一种天然的油溶性多酚化合物，具有强大的抗癌、抗炎和抗氧化活性。其游离形式由于溶解度极低，在肠道中吸收很差。使用纳米乳剂作为载体是提高姜黄素生物利用度的可行方法。为此，选择用于稳定纳米乳剂的乳化剂对于实现所需功能至关重要。
将磷脂酰胆碱（PC）和富含中链脂肪酸（42.5摩尔%）并与甘油作为助表面活性剂组合的磷脂酰胆碱（PCE）分别用于制备水包油纳米乳剂，编码为NEPC和NEPCE。
与NEPC相比，NEPCE的平均液滴尺寸显著更小（30纳米），包封率相同（100%），液滴稳定性更好，在储存时间（120天，4℃）内包封效率损失更低（3%）。以姜黄素浓度-时间曲线下面积和姜黄素血浆最大浓度衡量的生物利用度，总体而言，NEPCE显著高于NEPC和姜黄素粗水悬浮液（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。
这些数据支持富含中链脂肪酸的磷脂酰胆碱在提高纳米乳剂治疗应用生物利用度方面的作用。
