Department of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, Chnia.
Key Laboratory of Xin'an Medicine, Hefei 230038, China.
Nanomedicine (Lond). 2018 Feb;13(3):269-282. doi: 10.2217/nnm-2017-0277. Epub 2018 Jan 17.
The aim of this work was to optimize a nanoemulsion formulation and explain its absorption mechanism in improving the oral bioavailability of paeonol.
The bioavailability of paeonol was compared between paeonol nanoemulsion group and paeonol suspension group. The in situ single-pass intestine perfusion method, in vitro everted gut sacs method, Western blot analysis and Caco-2 cell transport studies were used to investigate the absorption mechanism of nanoemulsion.
Nanoemulsion was proved to enhance the bioavailability of paeonol. P-glycoprotein (P-gp) mediated efflux might be the main reason affecting the oral absorption of paeonol. The prepared nanoemulsion prevented the P-gp-mediated efflux and enhanced the bioavailability of paeonol.
The overall results revealed that nanoemulsion was an effective vehicle to improve the oral bioavailability of paeonol which resulted from the prevention of P-gp efflux probably.
本工作旨在优化纳米乳制剂配方，并解释其吸收机制，以提高丹皮酚的口服生物利用度。
比较丹皮酚纳米乳组和丹皮酚混悬液组的生物利用度。采用原位肠灌流法、外翻肠囊法、Western blot 分析和 Caco-2 细胞转运研究，探讨纳米乳的吸收机制。
纳米乳被证明能提高丹皮酚的生物利用度。P 糖蛋白（P-gp）介导的外排可能是影响丹皮酚口服吸收的主要原因。所制备的纳米乳能防止 P-gp 介导的外排，从而提高丹皮酚的生物利用度。
总体结果表明，纳米乳是一种有效的载体，可提高丹皮酚的口服生物利用度，这可能是由于其能防止 P-gp 外排。
