Guangdong Provincial Key Laboratory of Nutraceuticals and Functional Foods, College of Food Science, South China Agricultural University, Guangzhou 510642, Guangdong, PR China.
Guangdong Provincial Key Laboratory of Nutraceuticals and Functional Foods, College of Food Science, South China Agricultural University, Guangzhou 510642, Guangdong, PR China.
Food Res Int. 2024 Jan;175:113631. doi: 10.1016/j.foodres.2023.113631. Epub 2023 Oct 26.
Emulsions offer a promising approach for enhancing the bioavailability of lipophilic active compounds when administered orally. Nonetheless, the impact of lipid matrix composition on the efficacy of penetration and bioavailability remains uncertain. This research investigated the effects of solid lipid ratio in emulsions on colloidal stability, mucus permeability, and bioavailability in vivo. To assess colloidal stability in the gastrointestinal tract (GIT), Turbiscan was employed. The results indicated that an elevated solid lipid ratio improved intestinal stability through the formation of aggregations that resisted pancreatic absorption, as confirmed by TEM. The absorption in various intestinal sections was tested using the Ussing Chamber model. Notably, emulsion with 0 % solid lipid (G0M10) exhibited the highest cumulative permeation across the duodenum (221.2 ± 21.19 ng), jejunum (713.1 ± 20.93 ng), and ileum (1056.3 ± 392.06 ng) due to its higher in vitro release rate (>60 %) and smaller particle size. The cumulative permeation decreased with increasing solid lipid ratio. CLSM revealed that emulsions with a solid lipid ratio exceeding 50 % exhibited poor mucus permeability within 15 min due to aggregation during the passage in the GIT. However, over an extended penetration time (30 min), higher permeability was observed, reaching approximately 30 μm. In vitro release studies indicated that a higher solid lipid ratio resulted in a reduced release rate of curcumin (<60 %) compared to G0M10 (66.9 ± 3.58 %). Correlation analysis unveiled a positive link between bioavailability and in vitro release rate, while a negative correlation emerged with the solid lipid ratio. This work underscores the significance of solid lipid ratios in emulsions for optimizing bioavailability through their influence on stability, permeability, and release of lipophilic compounds in the GIT.
乳剂为提高亲脂性活性化合物经口服给药的生物利用度提供了一种很有前途的方法。然而，脂质基质组成对渗透效率和生物利用度的影响仍不确定。本研究考察了乳剂中固体脂质比例对胶体稳定性、粘液渗透性和体内生物利用度的影响。为了评估胃肠道 (GIT) 中的胶体稳定性，使用了 Turbiscan。结果表明，通过形成抵抗胰腺吸收的聚集物，提高固体脂质比例可以改善肠道稳定性，这得到了 TEM 的证实。使用 Ussing 室模型测试了各个肠段的吸收情况。值得注意的是，由于较高的体外释放率 (>60%)和较小的粒径，0%固体脂质的乳剂 (G0M10) 在十二指肠 (221.2±21.19ng)、空肠 (713.1±20.93ng) 和回肠 (1056.3±392.06ng) 中具有最高的累积渗透量。随着固体脂质比例的增加，累积渗透量逐渐减少。CLSM 显示，固体脂质比例超过 50%的乳剂在 GIT 中通过时由于聚集而在 15 分钟内表现出较差的粘液渗透性。然而，在较长的渗透时间 (30 分钟) 内，观察到较高的渗透性，达到约 30μm。体外释放研究表明，与 G0M10(66.9±3.58%)相比，较高的固体脂质比例导致姜黄素的释放率降低(<60%)。相关分析显示生物利用度与体外释放率之间存在正相关，而与固体脂质比例之间存在负相关。这项工作强调了乳剂中固体脂质比例在通过影响亲脂性化合物在 GIT 中的稳定性、渗透性和释放来优化生物利用度方面的重要性。
