Affiliation:
1. Department of Pharmacy, The Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, 250011, China
2. College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China
Abstract
Background:
Baicalein (BA) is a flavonoid extract from the root of Scutellaria baicalensis
Georgi with excellent biological activities, such as antioxidant and anti-inflammatory activities. However,
its poor water solubility limits its further development.
Objective:
This study aims to prepare BA-loaded Solutol HS15 (HS15-BA) micelles, evaluate the bioavailability,
and explore protective effects on carbon tetrachloride (CCl4) induced acute liver injury.
Methods:
The thin-film dispersion method was used to prepare HS15-BA micelles. The physicochemical,
in vitro release, pharmacokinetics, and hepatoprotective effects of HS15-BA micelles were studied.
Results:
The optimal formulation showed a spherical shape by characterization of the transmission electron
microscope (TEM) with an average small size (12.50 nm). The pharmacokinetic results illustrated
that HS15-BA increased the oral bioavailability of BA. The in vivo results showed that HS15-BA micelles
significantly inhibited the activity of the CCl4-induced liver injury marker enzymes aspartate
transaminase (AST) and alanine transaminase (ALT). Also, CCl4 induced oxidative damage to liver
tissue, leading to increased L-glutathione (GSH) and superoxide dismutase (SOD) activity and decreased
malondialdehyde (MDA) activity, while HS15-BA significantly reversed the above changes.
Moreover, BA also had a hepatoprotective effect through anti-inflammatory activity; the results of ELISA
and RT-PCR revealed that HS15-BA pretreatment significantly inhibited the increase in the expression
of inflammatory factors induced by CCl4.
Conclusion:
In summary, our study confirmed that HS15-BA micelles enhanced the bioavailability of
BA, and showed hepatoprotective effects through antioxidant and anti-inflammatory activities. HS15
could be considered a promising oral delivery carrier in treating liver disease.
Publisher
Bentham Science Publishers Ltd.