Pharmacokinetics of Panaxynol in Mice

Abstract

The purpose of our study is to explore the pharmacokinetic parameters of panaxynol (PA) and understand its potential and dosage used in pre-clinical animal models. For in vitro analysis,5 μM of PA was added to liver microsomes of mouse and human species. Nicotinamide adenine dinucleotide phosphate was added to initiate enzyme reaction except for the negative control. Liquid chromatography with tandem mass spectrometry (LC-MS/MS) analysis was used to measure concentrations. For in vivo studies, CD-1 mice were treated with PA by intravenous (IV) injection or oral administration (PO). Concentrations of PA were measured in plasma and tissue using LC-MS/MS. Pharmacokinetic parameters were obtained using non-compartmental analysis. Area under the curve concentration versus time was calculated using a linear trapezoidal model. In vitro , PA’s half-life is 21.4 min and 48.1 min in mouse and human liver microsomes, respectively. In vivo , PA has a half-life of 1.5 hr when IV-injected, and 5.9 hr when administered via PO, with a moderate bioavailability of 50.4%. Mice show no signs of toxicity up to 300 mg/kg PO. PA concentrations were highest in colon tissue 2 hr post-treatment at 486 ng/g of colon tissue.PA’s pharmacokinetic properties and low toxicity point to the safety and compatibility of PA with mice.

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“…Considering the % doping of Cy5.5-PEG2000-DSPE in the nanoparticle suspension, concentration of T-ZAPL75C nanoparticle was calculated and plotted against time (Figure b). The curve was then fitted and the concentration at zero-time, the elimination rate constant, the volume of distribution, the elimination half-life, and the clearance , were determined for the T-ZAPL75C nanoparticles. The values are mentioned in the table shown in Figure c.…”

Pathways Affected by Falcarinol-Type Polyacetylenes and Implications for Their Anti-Inflammatory Function and Potential in Cancer Chemoprevention

“…A plasma analysis of FaOH after oral administration showed that the compound’s concentration quickly reached a maximum of 1.72 μg/mL in 1 h. The plasma concentration then decreased in a multiphasic manner, reaching a final measurable concentration of 32.2 ng/mL after 24 h. FaOH had a half-life of 1.5 h when IV injected and 5.9 h when administered orally, with a bioavailability of 50.4%. The mice did not show any toxicity up to 300 mg/kg orally [ 132 ]. When mice were orally given 20 mg/kg of FaOH, the FaOH concentrations in the colon tissue were the highest at 2 h after treatment at 121 ng/mL [ 132 ].…”

“…The mice did not show any toxicity up to 300 mg/kg orally [ 132 ]. When mice were orally given 20 mg/kg of FaOH, the FaOH concentrations in the colon tissue were the highest at 2 h after treatment at 121 ng/mL [ 132 ]. The very high murine values contrast remarkably with the similarity of the maximal plasma concentration ranges reported in the above two human studies.…”