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Fabrication and Optimization of Self‐Microemulsions to Improve the Oral Bioavailability of Total Flavones of Hippophaë rhamnoides L

Guo, Ruixue, Guo, Xinbo, Hu, Xiaodan, Abbasi, Arshad Mehmood, Zhou, Lin, Li, Tong, Fu, Xiong, Liu, Rui Hai
Journal of food science 2017 v.82 no.12 pp. 2901-2909
absorption, bioavailability, droplet size, drug delivery systems, flavones, functional foods, ingredients, nanotechnology, oral administration, rats, solubility
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.