Abstract
Cardiovascular and metabolic disease (CMD) remains a main cause of premature death worldwide. Berberine (BBR), a lipid-lowering botanic compound with diversified potency against metabolic disorders, is a promising candidate for ameliorating CMD. The liver is the target of BBR so that liver-site accumulation could be important for fulfilling its therapeutic effect. In this study a rational designed micelle (CTA-Mic) consisting of α-tocopheryl hydrophobic core and on-site detachable polyethylene glycol-thiol shell is developed for effective liver deposition of BBR. The bio-distribution analysis proves that the accumulation of BBR in liver is increased by 248.8% assisted by micelles. Up-regulation of a range of energy-related genes is detectable in the HepG2 cells and in vivo. In the high fat diet-fed mice, BBR-CTA-Mic intervention remarkably improves metabolic profiles and reduces the formation of aortic arch plaque. Our results provide proof-of-concept for a liver-targeting strategy to ameliorate CMD using natural medicines facilitated by Nano-technology.
Highlights
Cardiovascular and metabolic disease (CMD) remains a main cause of premature death worldwide
The morphological feature of BBR-CTA-Mic confirmed that most of BBR was distributed within the hydrophobic core and along the surfactant molecules in certain intermediate positions within the micelle’s corona (Supplementary Fig. 2A)
Our results showed that BBR-CTA-Mic intervention (50 mg kg−1 day−1 of BBR) could improve high fat diet (HFD) induced metabolism disorders, lead to improvement of atherosclerosis
Summary
Cardiovascular and metabolic disease (CMD) remains a main cause of premature death worldwide. In this study a rational designed micelle (CTA-Mic) consisting of α-tocopheryl hydrophobic core and on-site detachable polyethylene glycol-thiol shell is developed for effective liver deposition of BBR. Mic) was developed in an attempt to facilitate the effective liver accumulation of BBR. This novel system consists of a D-αtocopheryl hydrophobic core and an on-site detachable crosslinked polyethylene glycol-thiol shell. The purpose of this study was to design and investigate the efficacy of BBR-CTA-Mic (50 mg kg−1 day−1 of BBR) on the treatment of CMD in the high fat diet (HFD)-fed mice
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