Self-emulsifying preconcentrates of daidzein-phospholipid complex: design, in vitro and in vivo appraisal.
Self-emulsifying phospholipid-complex preconcentrates (SEPPs) were fabricated to improve oral bioavailability of daidzein (DAI), an anticancer drug with challenging amphiphobic nature and extensive presystemic metabolism.



DAI-phosphatidylcholine complex was prepared to enhance DAI lipophilicity and loading in SEPPs. The physicochemical characteristics and the pharmacokinetic behavior in rats were studied.



Surfactant-free SEPP (plain DAI:Phosal®53MCT complex) was monodisperse upon aqueous dilution with nanorange globule size (485 ± 15 nm). Compared with drug suspension, it showed enhanced drug release and 2.38-fold enhanced oral bioavailability with minimized drug-induced intestinal irritation. Addition of 30% surfactant/co-surfactant mixture did not show any significant difference in drug release rate or absorption profile.



The highly safe surfactant-free SEPP could be an effective approach to improve DAI oral bioavailability.
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.|Department of Pharmaceutics, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
Yosra Sr
YS
Elnaggar
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Eman Mm
EM
Shehata
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Sally
S
Galal
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Ossama Y
OY
Abdallah
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D065546:Drug Liberation; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007529:Isoflavones / Q000737:chemistry / Q000494:pharmacology*; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology
D004655:Emulsions; D007529:Isoflavones; D010743:Phospholipids; D013501:Surface-Active Agents; C004742:daidzein
daidzein–phospholipid complex; oral bioavailability; self-emulsifying preconcentrate