Study on mechanism of transdermal administration of eugenol for pain treatment by network pharmacology and molecular docking technology.

The objective of this study was to explore the pharmacological mechanism of transdermal administration of eugenol (EUG) for pain treatment. Firstly, network pharmacology techniques were employed to identify the potential targets responsible for the analgesic effect of EUG. Subsequently, molecular docking technology was used to validate interactions between EUG and the crystal structure of the core target protein. Finally, the impact of EUG on the expression and activation of TRPV1 receptors in HaCaT cells was evaluated through in vitro experiments, thus confirming the analysis of network pharmacology. The study suggested that the transdermal administration of EUG for pain treatment might target the TRPV1 receptor. Molecular docking revealed that EUG could spontaneously bind to the TRPV1 receptor with a high binding ability. The analysis of Western blot (WB) and intracellular Ca2+ levels demonstrated that EUG could increase the expression of TRPV1 in HaCaT cells, activating TRPV1 to induce intracellular Ca2+ influx (P < 0.05). These findings suggested that the initial application of EUG would cause a brief stimulation of TRPV1 receptors and upregulation of TRPV1 expression. Upon continued exposure, EUG would act as a TRPV1 agonist, increasing intracellular Ca2+ levels that might be associated with desensitization of pain sensations.

High resveratrol-loaded microcapsules with trehalose and OSA starch as the wall materials: Fabrication, characterization, and evaluation.

To improve the solubility and stability of resveratrol (Res), Res nanocrystals (Res-ncs) as the capsule core were prepared by wet milling using hydroxypropyl methyl cellulose (HPMCE5), sodium dodecyl sulfate (SDS), and polyvinylpyrrolidone (PVPK30) as stabilizers, along with trehalose and octenyl succinic anhydride (OSA) modified starch were used as the wall material to produce Res microcapsules (Res-mcs) via spray drying. The fresh-prepared Res-ncs and rehydrated Res-mcs had mean particle sizes of 190.30 ± 3.43 and 204.70 ± 3.60 nm, zeta potentials of -13.90 ± 0.28 and - 11.20 ± 0.34 mV, and the loading capacities (LC) were as high as 73.03 % and 28.83 %. Particle morphology showed that Res-mcs had more regular and smooth spherical structures. FTIR indicated that Res may have hydrogen bonding with the walls. XRD and DSC exhibited that Res in nanocrystals and microcapsules existed mostly as amorphous structures. The solubility of Res-mcs and Res-ncs was increased, with excellent redispersibility and rapid dissolution of Res in vitro. The antioxidant properties of Res-mcs were protected and improved. With the walls acting as a physical barrier, Res-mcs have better photothermal stability than raw Res. Res-mcs have a relative bioavailability of 171.25 %, which is higher than that of raw Res.

[Kinetic turbidimetric limulus assay of bacterial endotoxin in the replacement solution of on-line hemodiafiltration].

OBJECTIVE: To determine bacterial endotoxin in the replacement solution of on-line hemodiafiltration (on-line HDF) using kinetic turbidimetric limulus test. METHODS AND RESULTS: Validation test was performed with the replacement solution of on-line HDF in which quantified standard endotoxin was added. The recovery rates of endotoxin from the replacement solution and its dilutions at 1/5, 1/10, and 1/20 were 58.17%, 106.7%, 99.00% and 98.79%, respectively, suggesting that the optimal dilution was at 1/10. Standard endotoxin was added into the replacement solution of on-line HDF of 3 batches (040408, 040511,040527), and the recovery rates in their dilution at 1/10 were 76.32%, 99.00% and 96.24%, respectively. The standard endotoxin in the working curve was 1.00, 0.125, and 0.0156 Eu/ml (endotoxin unit/ml), and the dilution at 1/10 of the replacement solution is effective to eliminate the interference in limulus test. CONCLUSION: Kinetic turbidimetric limulus test provide a means to detect endotoxin in the replacement solution of on-line HDF.