A self-assembled nanodelivery system enhances the oral bioavailability of daidzein: in vitro characteristics and in vivo performance.
OBJECTIVE
A self-assembled nano-based delivery system was designed and developed to increase the oral bioavailability of poor hydrophilic and lipophilic daidzein.


METHODS
Daidzein was firstly combined with lecithin to form the daidzein-lecithin complex, then self-assembled into micelles (DLMs) with lecithin and sodium bile. The physiochemical properties and intestinal absorption of DLMs were characterized, and the pharmacokinetic behavior was evaluated in rats.


RESULTS
DLMs exhibited nanometer-sized particles. DLMs were mainly distributed in the stomach and proximal intestine after oral administration. The intestinal absorption of DLMs was significantly improved, and DLMs could be absorbed via both endocytosis and passive transport. The AUC(0-t) value of daidzein in rats treated with DLMs was ninefold greater than that of free daidzein suspension.


CONCLUSIONS
The presented delivery system could provide a new promising strategy for enhancing the oral bioavailability of drugs with poor hydrophilicity and lipophilicity.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Zhiwen
Z
Zhang
Yan
Y
Huang
Fang
F
Gao
Zhiwei
Z
Gao
Huihui
H
Bu
Wangwen
W
Gu
Yaping
Y
Li
D000284:Administration, Oral; D000818:Animals; D004705:Endocytosis / Q000502:physiology; D007408:Intestinal Absorption; D007529:Isoflavones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
D007529:Isoflavones; C004742:daidzein