Evaluation of the distribution of piperine in brain, plasma and cerebrospinal fluid after oral administration in rat
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AbstractIntroduction. Piperine, the biological active component in black pepper, served several pharmacologic actions on central nervous system, such as anti-depression, anti-convulsion and neurodegeneration protection. However, the brain uptake pharmacokinetics of piperine and its brain distribution have never been studied.
Aims. To investigate the pharmacokinetics of piperine in brain, plasma and cerebrospinal fluid (CSF) after its oral administration and to evaluate the distribution of piperine in different brain regions.
Methods. For pharmacokinetic study, piperine was administered orally to SD rats at two different doses (3.5 and 35 mg/kg). The rats were sacrificed at different time intervals (0.25, 0.5, 1, 2, 4, 6, 8 and 10 h for low dose group, 0.5, 1, 2, 4, 6, 16, 20 and 24 h for high dose group; n=5 for each time interval) to collect plasma, brain and CSF samples. The collected brain samples in high dose group were dissected into different anatomical regions. The piperine concentrations in collected samples were analyzed by LC-MS/MS and unbound fractions of piperine in plasma and brain were determined by equilibrium dialysis. Besides, the unbound volume of distribution in the brain (Vu,brain) was determined by brain slice method.
Results. Piperine has demonstrated similar concentrations versus time profiles in brain and plasma after oral administrations, with brain to plasma AUC0→∞ ratios close to 1. CSF concentrations of piperine were much lower than that in brain and plasma. Piperine showed high affinity towards brain tissue (97.55-98.06%) and plasma protein (96.22-97.77%) with a Vu,brain of 29.79±0.94 ml/g. The unbound brain to plasma AUC0→∞ ratios was 1.31~1.49 for both dose groups, suggesting a high brain penetration of piperine that leads to its evenly distribution in different brain regions.
Discussion. Piperine with high affinity towards brain and plasma could efficiently and homogenously distribute to brain after oral administration. [CUHK 7010298]
All Author(s) ListTianjing Ren, Qianwen Wang, Zhong Zuo
Name of Conference12th International Conference on Cerebral Vascular Biology 2017
Start Date of Conference28/11/2017
End Date of Conference01/12/2017
Place of ConferenceMelbourne
Country/Region of ConferenceAustralia
LanguagesEnglish-United States

Last updated on 2018-22-06 at 15:07