Hepatic targeting of glycyrrhetinic acid via nanomicelles based on stearic acid-modified fenugreek gum

Abstract

This study aimed to increase the solubility of glycyrrhetinic acid (GA) in water and enhance its liver-targeting ability using self-assembling nanomicelles (NMs) based on stearic acid-modified fenugreek gum . The GA/FG-C 18 NMs were prepared by an ultrasonication dispersion method. The nanomicelles were spherical particles with a particle size of 198.61 ± 1.58 nm and a zeta potential of À30.12 ± 0.28 mV. The drug loading and encapsulation efficiency were 13.34 ± 0.24% and 80.07 ± 1.44%, respectively. The results of differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) indicated that GA was successfully encapsulated into the nanomicelles in a molecularly dispersed state. An in vitro release test showed that GA/FG-C 18 NMs possessed a slow drug release profile in PBS (pH 7.4) over 200 h. The cytotoxicity assay indicated that GA/FG-C 18 NMs showed much higher inhibitory efficacy in HepG2 cells than in MCF-7 cells. Tissue section studies indicated that the accumulation of DiR-loaded FG-C 18 nanomicelles in the liver of mice was higher than that of the DiR solution, and the fluorescence intensity decreased over time. GA/FG-C 18 NMs showed a larger area under the curve (AUC) and mean residence time (MRT) compared with free GA after intravenous administration in mice. The in vivo studies showed that GA mainly accumulated in the liver after encapsulation by FG-C 18 NMs, and the drug concentration was higher than that of free GA. These results suggested that FG-C 18 NMs could serve as a potential drug delivery system for targeting GA to liver tissue.

Construction of targeted drug-loaded composite polysaccharide hydrogels and verification of anti-tumor effect in vitro

“…The apparent viscosity of FA-ASA-FG/MTX was higher than that of SA/MTX because FG might interpenetrate the hydrogel network, which further proves that FA-ASA-FG/MTX had a denser network structure. 29 The above results confirmed the successful preparation of drug-loaded hydrogels, and showed that FA-ASA-FG/MTX had a high complex viscosity and apparent viscosity.…”

Calorimetric Evaluation of Glycyrrhetic Acid (GA)- and Stearyl Glycyrrhetinate (SG)-Loaded Solid Lipid Nanoparticle Interactions with a Model Biomembrane

“…This behaviour was confirmed by the release studies (data not shown); SG was not released from the nanocarriers due to its extremely lipophilic structure (insoluble). On the other hand, GA-SLNs showed poor release due to the less lipophilic nature of GA compared to SG (<0.01 mg/mL) [ 28 ].…”