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 Cmax and 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-t of 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.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Zhang Y,He L,Yue S,Huang Q,Zhang Y,Yang J

doi

10.1080/10717544.2017.1284946

subject

Has Abstract

pub_date

2017-11-01 00:00:00

pages

632-640

issue

1

eissn

1071-7544

issn

1521-0464

journal_volume

24

pub_type

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