Supersaturable Self-Emulsifying Drug Delivery System of Krill Oil with Improved Oral Absorption and Hypotriglyceridemic Function
Supersaturable Self-Emulsifying Drug Delivery System of Krill Oil with Improved Oral Absorption and Hypotriglyceridemic Function
复制标题
具有改善口服吸收和降甘油三酯功能的磷虾油过饱和自乳化给药系统
DOI：
10.1021/acs.jafc.8b00693
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发表时间：
2018
影响因子：
6.1
通讯作者：
Onoue Satomi
中科院分区：
文献类型：
--
作者：
Seto Yoshiki;Morizane Chikara;Ueno Kodai;Sato Hideyuki;Onoue Satomi
本研究旨在开发富含二十二碳六烯酸和二十碳五烯酸（EPA）的磷虾油（KO）的过饱和自乳化药物递送系统（S-SEDDS），以改善其降甘油三酯功能。通过添加溶血卵磷脂、甘油和羟丙基甲基纤维素 (HPMC) 制备 KO 的 S-SEDDS (KO/S-S-SEDDS)。还制备了 KO 自乳化给药系统 (KO/SEDDS) 和 KO 与 HPMC (KO/HPMC) 的自乳化给药系统用于比较。对 KO 样品的理化和药代动力学特性进行了表征，并评估了 KO/S-SEDDS 的降甘油三酯功能。 KO/SEDDS 和 KO/S-SEDDS 中的微粉化液滴，平均直径为 ca.与 KO 和 KO/HPMC 相比，可以观察到 270 nm。 KO/HPMC 和 KO/S-SEDDS 均倾向于增强 KO 的溶出行为，并且 S-SEDDS 配方由于微粉化液滴和 HPMC 的添加而改善了 KO 的溶出行为。根据 EPA 的药代动力学分析，KO/S-SEDDS（60 mg EPA/kg）改善了 KO 的口服吸收，与口服 KO 相比，连续 7 天重复口服 KO/S-SEDDS（250 mg KO kg–1day–1）对玉米油诱导的高甘油三酯血症大鼠具有有效的降甘油三酯作用。基于这些发现，S-SEDDS 方法可能是增强 KO 营养保健特性的有效剂量选择。
This study aimed to develop a supersaturable self-emulsifying drug delivery system (S-SEDDS) of krill oil (KO), a rich source of docosahexaenoic acid and eicosapentaenoic acid (EPA), to improve its hypotriglyceridemic function. S-SEDDS of KO (KO/S-SEDDS) was prepared by the addition of lysolecithin, glycerin, and hydroxypropyl methylcellulose (HPMC). Self-emulsifying drug delivery system of KO (KO/SEDDS) and KO with HPMC (KO/HPMC) were also prepared for comparison purposes. The physicochemical and pharmacokinetic properties of KO samples were characterized, and the hypotriglyceridemic function of KO/S-SEDDS was evaluated. Micronized droplets in KO/SEDDS and KO/S-SEDDS with a mean diameter of ca. 270 nm could be observed in comparison to KO and KO/HPMC. Both KO/HPMC and KO/S-SEDDS tended to enhance the dissolution behavior of KO, and the S-SEDDS formulation improved the dissolution behavior of KO as a result of micronized droplets and the addition of HPMC. KO/S-SEDDS (60 mg of EPA/kg) improved the oral absorption of KO based on the pharmacokinetic profiling of EPA, and repeated oral administration of KO/S-SEDDS (250 mg of KO kg–1day–1) for 7 days had a potent hypotriglyceridemic effect on rats with corn-oil-induced hypertriglyceridemia compared to orally administered KO. On the basis of these findings, the S-SEDDS approach might be an efficacious dosage option to enhance the nutraceutical properties of KO.