To improve the efficiency of drug delivery, a mannose vinyl stearate mannose ligand (Man ligand) with active liver-targeting properties was synthesized.

Non-aqueous enzymatic synthesis was used to modify the structure of mannose. Glycyrrhetinic acid-tanshinone lipid nanoparticles (GT-LN) and liver-targeted glycyrrhetinic acid-tanshinone mannose-modified lipid nanoparticles (GT-MLN) were prepared. The physicochemical properties and release profiles of both formulations were evaluated, and their pharmacokinetic behavior and tissue distribution were investigated.

The average particle sizes of GT-LN and GT-MLN were 190.20 ± 1.35 and 204.83 ± 3.86 nm, respectively, with corresponding surface Zeta potentials of −28.0 ± 1.68 and −30.24 ± 2.10 mV. The drug release profile of GT-LN conformed to the Higuchi equation, whereas that of GT-MLN followed both the first-order kinetic and Ritger–Peppas equations. Both formulations significantly enhanced the gastrointestinal stability of the drug. In vivo studies in mice demonstrated that hepatic GA and TSN concentrations in both groups were significantly higher than those in the original drug suspension group (P = .01). Notably, the concentrations in the GT-MLN group were significantly higher compared to the GT-LN group (P = .01).

Man ligand was formed via the linkage of vinyl stearate with the hydroxyl group at C-6 in mannose. The Man ligand endowed these lipid nanoparticles with obvious active liver-targeting properties. Our results provide an efficient and stable route of drug delivery to the liver with improved drug availability.

The aim of this study was to discover the potential biomarkers changes on a rat model of isoproterenol (ISO) induced myocardial ischaemia before and after treatment with a Xiangdan submicron emulsion and to explore the unclearing mechanisms by urinary metabolomics.

Three active traditional Chinese medicine (TCM) ingredients were formulated into a lyophilized submicron emulsion powder with hydroxypropyl-β-cyclodextrin encapsulation by high pressure homogenization technology. The three ingredients were given both separately and combined, and the corresponding effects of the three drugs were compared. Principal component analysis (PCA) and the HPLC-UV analytical method was applied to explore the change of composition of urine metabolites in a rat model of isoproterenol induced myocardial ischaemia.

Analytical methods measuring the three active ingredients in urine samples were established. PCA score plots revealed that the therapeutic effect of the Xiangdan submicron emulsion was more significant than that of the Xiangdan injection. There was a synergistic effect among the three active ingredients. Furthermore, studies of rat metabolism changes and structure analysis of biological markers indicated that the mechanism of Xiangdan formulations was related to the inhibition of abnormal tryptophan metabolism.

Xiangdan preparations had a confirmed effect in the treatment of coronary heart disease, especially with the novel Xiangdan submicron emulsion formulation. Urinary metabolomics methods to monitor special biomarker changes is an excellent method to reveal the mechanism of action of TCM drugs.