title: Self-micro emulsifying formulation improved intestinal absorption and oral bioavailability of bakuchiol.
abstract: Bakuchiol (BAK), isolated from the seeds of Psoralea corylifolia L., recently presents a variety of pharmacologic activities. However, the poor oral bioavailability limits its further development and clinical use. The purpose of this study was to establish a self-microemulsifying (SME) formulation for oral delivery improvement of BAK. The optimized liquid SME formulation was comprised of BAK (40 %), Cremophor RH 40 (30 %) and Labrasol (30 %). The emulsion droplets were spherical in shape, and particle size and zeta potential were determined. The in vitro dissolution test of BAK-SME formulation illustrated faster dissolution rate than the bulk drug. The permeabilities of 40 μg mL-1BAK-SME formulation in rat intestinal segments of duodenum, jejunum, ileum and colon were 30.91 × 10-3, 23.61 × 10-3, 29.43 × 10-3and 23.62 × 10-3cm min-1, respectively, exhibiting 3.99 times in duodenum, 2.59 times in ileum and 2.31 times in colon greater than BAK perfusate. The oral bioavailability of BAK-SME formulation at a dose of 150 mg kg-1was determined in rats. The Cmaxand the AUC(0-24h)were 515.4 ng mL-1and 4,327.2 h ng mL-1, respectively, which were 1.90 fold and 1.73 fold greater than the value of BAK suspension. All these results clearly stated that BAK-SME formulation performed well-improvement on oral bioavailability of BAK.
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, People's Republic of China.
authors.forename: Jiaxin
authors.initials: J
authors.lastname: Pi
authors.forename: Xu
authors.initials: X
authors.lastname: Gao
authors.forename: Yue
authors.initials: Y
authors.lastname: Yu
authors.forename: Yin
authors.initials: Y
authors.lastname: Zheng
authors.forename: Zhuangzhi
authors.initials: Z
authors.lastname: Zhu
authors.forename: Yajing
authors.initials: Y
authors.lastname: Wang