The purpose of this work was to improve the oral bioavailability of a poorly soluble functional food ingredient, the total flavones of Hippophaë rhamnoides L. (TFH). A self-microemulsion drug delivery system (SMEDDS) was developed to overcome the problems of poor absorption of TFH in vivo. The optimal SMEDDS significantly enhanced the solubility of TFH up to 530 times compared to that in water. The mean droplet size was 61.76 nm with uniform distribution. And the loaded system was stable at 25 °C for 3 mo with transparent appearance. The in vitro release of TFH from SMEDDS was faster and more complete than that from suspension. After oral administration of TFH-SMEDDS in rats, the relative bioavailability of TFH was dramatically improved for 3.09 times compared with the unencapsulated form. The investigation indicated the potential application of SMEDDS as a vehicle to improve the oral bioavailability of TFH. PRACTICAL APPLICATION The lipid-based nanotechnology, namely self-microemulsion drug delivery system (SMEDDS) was used to improve the bioavailability and oral delivery of total flavones of Hippophaë rhamnoides L. (TFH). The relevant bioavailability of TFH could be remarkably 3-fold improved by the optimized SMEDDS. The SMEDDS produced via a simple one-step process for poorly soluble TFH to achieve a significant improvement in the bioavailability, may endorse the promising utilization of TFH in functional foods as well as pharmaceutical fields with an enhanced absorption in vivo.

中文翻译：

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提高沙棘总黄酮口服生物利用度的自微乳液的制备与优化

这项工作的目的是提高难溶性功能性食品成分的口服生物利用度，即沙棘总黄酮 (TFH)。为了克服体内TFH吸收差的问题，开发了一种自微乳给药系统（SMEDDS）。与在水中相比，最佳 SMEDDS 显着提高了 TFH 的溶解度高达 530 倍。平均液滴尺寸为 61.76 nm，分布均匀。加载的系统在 25°C 下稳定 3 个月，外观透明。SMEDDS体外释放TFH比悬浮液更快、更完全。大鼠口服 TFH-SMEDDS 后，TFH 的相对生物利用度与未包封形式相比显着提高了 3.09 倍。调查表明 SMEDDS 作为提高 TFH 口服生物利用度的载体的潜在应用。实际应用 基于脂质的纳米技术，即自微乳给药系统（SMEDDS）被用于提高沙棘总黄酮（TFH）的生物利用度和口服给药。优化的 SMEDDS 可使 TFH 的相关生物利用度显着提高 3 倍。通过简单的一步法制备难溶性 TFH 的 SMEDDS 可显着提高生物利用度，这可能证明 TFH 在功能性食品和药物领域中具有增强的体内吸收的前景。即自微乳给药系统（SMEDDS）用于提高沙棘总黄酮（TFH）的生物利用度和口服给药。优化的 SMEDDS 可使 TFH 的相关生物利用度显着提高 3 倍。通过简单的一步法制备难溶性 TFH 的 SMEDDS 可显着提高生物利用度，这可能证明 TFH 在功能性食品和药物领域中具有增强的体内吸收的前景。即自微乳给药系统（SMEDDS）用于提高沙棘总黄酮（TFH）的生物利用度和口服给药。优化的 SMEDDS 可使 TFH 的相关生物利用度显着提高 3 倍。通过简单的一步法制备难溶性 TFH 的 SMEDDS 可显着提高生物利用度，这可能证明 TFH 在功能性食品和药物领域中具有增强的体内吸收的前景。