Food Nutrition and Health Program, Faculty of Land and Food Systems, The University of British Columbia, 2205 East Mall, Vancouver, BC, V6T 1Z4, Canada.
Ascension Sciences Inc, Vancouver, BC, Canada.
Sci Rep. 2021 Jan 8;11(1):72. doi: 10.1038/s41598-020-79161-w.
Emerging formulation technologies aimed to produce nanoemulsions with improved characteristics, such as stability are attractive endeavors; however, comparisons between competing technologies are lacking. In this study, two formulation techniques that employed ultrasound and microfluidic approaches, respectively, were examined for relative capacity to produce serviceable oil in water nanoemulsions, based on hempseed oil (HSO). The ultrasound method reached > 99.5% entrapment efficiency with nanoemulsions that had an average droplet size (Z-Ave) < 180 nm and polydispersity index (PDI) of 0.15 ± 0.04. Surfactant concentration (% w/v) was found to be a significant factor (p < 0.05) controlling the Z-Ave, PDI and zeta potential of these nanoparticles. On the other hand, the microfluidic approach produced smaller particles compared to ultrasonication, with good stability observed during storage at room temperature. The Z-Ave of < 62.0 nm was achieved for microfluidic nanoemulsions by adjusting the aqueous : organic flow rate ratio and total flow rate at 4:1 and 12 mL/min, respectively. Further analyses including a morphology examination, a simulated gastrointestinal release behavior study, transepithelial transport evaluations and a toxicity test, using a Caco2-cell model, were performed to assess the functionality of the prepared formulations. The results of this study conclude that both approaches of ultrasound and microfluidics have the capability to prepare an HSO-nanoemulsion formulation, with acceptable characteristics and stability for oral delivery applications.
旨在生产具有改进特性（如稳定性）的纳米乳液的新兴制剂技术是吸引人的努力；然而，缺乏对竞争技术的比较。在这项研究中，分别使用超声和微流控方法的两种制剂技术，根据大麻籽油（HSO），考察了相对生产油包水型纳米乳液的能力。超声法达到了>99.5%的包封效率，纳米乳液的平均粒径（Z-Ave）<180nm，多分散指数（PDI）为0.15±0.04。发现表面活性剂浓度（% w/v）是控制这些纳米颗粒的 Z-Ave、PDI 和 Zeta 电位的重要因素（p<0.05）。另一方面，与超声相比，微流控方法产生的颗粒更小，在室温下储存时观察到良好的稳定性。通过调整水相：有机流速比和总流速分别为 4:1 和 12mL/min，可实现微流控纳米乳液的 Z-Ave<62.0nm。进一步的分析，包括形态学检查、模拟胃肠道释放行为研究、跨上皮转运评估和使用 Caco2 细胞模型的毒性试验，用于评估所制备制剂的功能。这项研究的结果表明，超声和微流控两种方法都有能力制备大麻籽油纳米乳液制剂，具有可接受的特性和稳定性，适用于口服给药应用。
