Docosahexaenoic acid is a omega-3-fatty acid which together with other long-chain omega-3-fatty acid known to have protective effect against various diseases including hypertension, myocardial infarction, Alzheimer disease, and cancers. Poor bioavailability owning to limited aqueous solubility limits its effective therapeutic delivery. Self-nanoemulsifying drug delivery systems are known to enhance the systemic absorption of poorly bioavailable lipophilic bioactive/therapeutics compounds. The purpose of this work was to investigate the potential of self-nanoemulsifying drug delivery systems produced by spontaneous nanoemulsification to enhance the oral bioavailability of docosahexaenoic acid. Initially, the screening of oil, surfactant, and cosurfactant was carried out by determining the miscibility and emulsifiability of the component with docosahexaenoic acid. Docosahexaenoic acid-containing self-nanoemulsifying drug delivery systems were prepared using Capryol 90, Tween 20, and polyethylene glycol 200 due to their excellent miscibility and emulsifiability with docosahexaenoic acid. Docosahexaenoic acid-containing self-nanoemulsifying drug delivery systems’ droplet size, size distribution, and zeta potential were found to be 111.5 ± 4.2 nm, 0.269 ± 0.05 nm, and −23.53 ± 2.9 mV, respectively. The in vitro drug release and ex vivo absorption studies showed better in vitro release and intestinal absorption as compared to docosahexaenoic acid aqueous dispersion. In vivo studies demonstrated a significant increase (p < 0.001) in the oral bioavailability of docosahexaenoic acid-containing self-nanoemulsifying drug delivery systems in comparison to a docosahexaenoic acid aqueous dispersion. This indicated the potential of self-nanoemulsifying drug delivery systems as an effective unit dosage form for the oral delivery of docosahexaenoic acid.

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含二十二碳六烯酸的口服自纳米乳化给药系统的配方设计及药代动力学评价

二十二碳六烯酸是一种 omega-3-脂肪酸，它与其他长链 omega-3-脂肪酸一起已知对多种疾病具有保护作用，包括高血压、心肌梗塞、阿尔茨海默病和癌症。由于有限的水溶性而导致的较差的生物利用度限制了其有效的治疗递送。已知自纳米乳化药物递送系统可增强生物利用度差的亲脂性生物活性/治疗化合物的全身吸收。这项工作的目的是研究自发纳米乳化产生的自纳米乳化药物递送系统在提高二十二碳六烯酸的口服生物利用度方面的潜力。最初，筛选油、表面活性剂、助表面活性剂通过测定组分与二十二碳六烯酸的混溶性和乳化性来进行。使用 Capryol 90、吐温 20 和聚乙二醇 200 制备含有二十二碳六烯酸的自纳米乳化给药系统，因为它们与二十二碳六烯酸具有优异的混溶性和乳化性。发现含有二十二碳六烯酸的自纳米乳化给药系统的液滴尺寸、尺寸分布和 zeta 电位分别为 111.5 ± 4.2 nm、0.269 ± 0.05 nm 和 -23.53 ± 2.9 mV。与二十二碳六烯酸水分散体相比，体外药物释放和离体吸收研究显示更好的体外释放和肠道吸收。体内研究表明显着增加（p < 0。001）与二十二碳六烯酸水分散体相比，含二十二碳六烯酸的自纳米乳化药物递送系统的口服生物利用度。这表明自纳米乳化药物递送系统作为二十二碳六烯酸口服递送的有效单位剂型的潜力。