Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University , Phitsanulok 65000 , Thailand.
Pharm Dev Technol. 2014 Sep;19(6):735-42. doi: 10.3109/10837450.2013.829092. Epub 2013 Aug 28.
A self-nanoemulsifying drug delivery system (SNEDDS) has been developed for enhanced oral bioavailability of lutein. Its permeation enhancement has been evaluated using monolayers of Caco-2 cells. SNEDDS is composed of a mixture of Lexol® and Emulmetik® 900, Labrasol®, and Tween 80 as oil, surfactant and co-surfactant, respectively. Upon dilution of lutein-loaded SNEDDS with water, a nanoemulsion was obtained in <10 s with spherical droplets of 40-150 nm in diameter. The zeta potential was in the range of -19 to -32 mV. Increasing the ratio of surfactant to co-surfactant decreased the mean droplet size. Dissolution studies showed that lutein was released rapidly (<5 min) from SNEDDS into 0.1 N HCl and pH 6.8 phosphate buffer solution without any aggregation. In vitro studies using Caco-2 cells revealed that lutein-loaded SNEDDS showed shorter lag time and greater (2-fold) cellular accumulation compared with the lutein dispersion.
已开发出自纳米乳化药物传递系统 (SNEDDS) 以提高叶黄素的口服生物利用度。使用 Caco-2 细胞单层评估了其渗透增强作用。 SNEDDS 由 Lexol®和 Emulmetik® 900、Labrasol®和 Tween 80 的混合物组成，分别为油、表面活性剂和助表面活性剂。将负载叶黄素的 SNEDDS 用水稀释后，在<10 s 内即可获得纳米乳液，其粒径为 40-150nm 的球形液滴。zeta 电位范围为-19 至-32 mV。增加表面活性剂与助表面活性剂的比例会降低平均液滴尺寸。溶解研究表明，SNEDDS 中的叶黄素在没有任何聚集的情况下迅速（<5 分钟）从 SNEDDS 释放到 0.1 N HCl 和 pH 6.8 磷酸盐缓冲溶液中。使用 Caco-2 细胞的体外研究表明，与叶黄素分散体相比，负载叶黄素的 SNEDDS 表现出更短的滞后时间和更高的（2 倍）细胞积累。
