Abstract
In this study, novel glycyrrhetinic acid (GA) liposomes modified with a liver-targeting galactosylated derivative ligand (Gal) were prepared using a film-dispersion method. To characterize the samples, particle size, zeta potential, drug loading, and encapsulation efficiency were performed. Moreover, plasma and tissues were pre-treated by liquid-liquid extraction and analyzed by high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). The results showed that the mean residence times (MRTs) and the area under the curve (AUC) of GA liposomes with Gal (Gal-GA-LP), and GA liposomes (GA-LP) were higher than the GA solution (GA-S) in plasma. The tissue (liver) distribution of Gal-GA-LP was significantly different in contrast to GA-LP. The relative intake rate (Re) of Gal-GA-LP and GA-LP in the liver was 4.752 and 2.196, respectively. The peak concentration ratio (Ce) of Gal-GA-LP and GA-LP in the liver was 2.796 and 1.083, respectively. The targeting efficiency (Te) of Gal-GA-LP and GA-LP in the liver was 48.193% and 34.718%, respectively. Taken together, the results indicate that Gal-GA-LP is an ideal complex for liver-targeting, and has great potential application in the clinical treatment of hepatic diseases. Drug loading and releasing experiments also indicated that most liposomes are spherical structures and have good dispersity under physiologic conditions, which could prolong GA release efficiency in vitro.
Highlights
Glycyrrhetinic acid (GA), serving as an active principal ingredient of glycyrrhizin, is hydrolyzed by glucuronidase after oral administration [1]
The results indicated that a suitable proportion of glycyrrhetinic acid (GA) could improve the encapsulation efficiency, as well as dispersity; the particle size decreased gradually when improving the GA proportion because that GA could be mixed uniformly with blank liposomes only when relatively saturated
A novel galactosylated derivates modified liposomes are designed for selective targeting of hepatic cells which are over-expressing asialoglycoprotein receptor
Summary
Glycyrrhetinic acid (GA), serving as an active principal ingredient of glycyrrhizin, is hydrolyzed by glucuronidase after oral administration [1]. GA has multi-beneficial pharmacologic activities, including anti-ulcerative [6], anti-inflammatory [7], anti-viral [8], and interferon induction [9]; GA is lipophilic and has low solubility in water (
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