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首页> 外文期刊>Biomolecules & therapeutics >Self-Nanoemulsifying Drug Delivery System of Lutein: Physico-chemical Properties and Effect on Bioavailability of Warfarin
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Self-Nanoemulsifying Drug Delivery System of Lutein: Physico-chemical Properties and Effect on Bioavailability of Warfarin

机译：叶黄素的自纳米乳化递药系统：华法林的理化性质及其对生物利用度的影响

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摘要

Objective of present study was to prepare and characterize self-nanoemutsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or I_utrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in C_(max) and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.
机译：本研究的目的是制备和表征叶黄素的自纳米化药物递送系统（SNEDDS），并评估其对华法林生物利用度的影响。 SNEDDS是使用油，表面活性剂和辅助表面活性剂根据拟三元相图制备的，具有最佳组成。使用Sprague Dawley大鼠进行SNEDDS对华法林生物利用度的影响。叶黄素通过将Peceol作为油，Labrasol作为表面活性剂以及Transcutol-HP或I_utrol-E400作为辅助表面活性剂的组合成功配制成SNEDDS，可立即自乳化和溶解。 15分钟后几乎完全溶解，而从叶黄素粉末或市售制剂的胶囊内含量检测不到叶黄素。叶黄素的SNEDDS制剂会影响华法林的生物利用度，显示大鼠中C_（max）和AUC的药物增加约10％，而叶黄素作为非SNEDDS不会改变这些参数。尽管尚未阐明确切的机理，但看来用于SNEDDS制剂的表面活性剂和助表面活性剂会引起小肠微绒毛的解剖结构紊乱，从而导致粘膜的通透性改变。基于此发现，建议谨慎使用治疗范围较窄的药物（如华法林），以避免由于SNEDDS中所含的大量表面活性剂而引起不良的药物相互作用。

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