title: Characterization and evaluation of a self-microemulsifying drug delivery system containing tectorigenin, an isoflavone with low aqueous solubility and poor permeability.
abstract: The purpose of this study was to characterize and evaluate tectorigenin-loaded self-microemulsifying drug delivery system (TG-SMEDDS), a previously studied preparation, and further confirm the improvement of TG in solubility and bioavailability. The appearance of TG-SMEDDS was clear and transparent, with good mobility. The microemulsion formed by TG-SMEDDS was globular, edge smooth, clear-cut, and distribution homogeneous under transmission electron microscope. The stability studies revealed that TG-SMEDDS remained stable at room temperature for at least 3 months. TG-SMEDDS showed excellent dissolution behavior that more than 90% of TG was released in only 5 min. The in situ intestinal perfusion studies indicated enhancement of absorption in four tested intestinal segments, and the main absorption site of TG was changed to duodenum. In addition, TG-SMEDDS showed significantly higher Cmaxand AUC values (11-fold and 5-fold higher values, respectively; P < 0.05) than TG, and the absolute oral bioavailability of TG-SMEDDS was 56.33% (5-fold higher than that of crude TG). What's more, the AUC0-tof crude TG and TG-SMEDDS in bile duct non-ligation rats were 6.05 and 2.80 times, respectively, than that in bile duct ligation rats, indicating the existence of enterohepatic circulation and the secretion of bile could significantly affect the absorption of TG. Further studies showed that even the bile duct was ligation, TG-SMEDDS can still keep a better oral bioavailability (179.67%, compared with crude TG in the bile duct non-ligation rats). Therefore, our study implies that SMEDDS containing TG could be an effective strategy for the oral administration of TG.
authors.affiliation: a West China School of Pharmacy, Sichuan University , Chengdu , China.
authors.forename: Yunrong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: b Chengdu Women and Children's Central Hospital , Chengdu , China , and.
authors.forename: Li
authors.initials: L
authors.lastname: He
authors.affiliation: b Chengdu Women and Children's Central Hospital , Chengdu , China , and.
authors.forename: Shanlan
authors.initials: S
authors.lastname: Yue
authors.affiliation: a West China School of Pharmacy, Sichuan University , Chengdu , China.
authors.forename: Qingting
authors.initials: Q
authors.lastname: Huang
authors.affiliation: c Medical College of China Three Gorges University , Yichang , China.
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: a West China School of Pharmacy, Sichuan University , Chengdu , China.
authors.forename: Junyi
authors.initials: J
authors.lastname: Yang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D001652:Bile Ducts / Q000601:surgery; D001682:Biological Availability; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004655:Emulsions; D004764:Enterohepatic Circulation; D007408:Intestinal Absorption; D007529:Isoflavones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008026:Ligation; D046529:Microscopy, Electron, Transmission; D010539:Permeability; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D004655:Emulsions; D007529:Isoflavones; C120039:tectorigenin
keywords: Tectorigenin; bioavailability; enterohepatic circulation; in situ gastric and intestine perfusion; self-microemulsifying drug delivery system