Comparative pharmacokinetic studies of borneol in mouse plasma and brain by different administrations

Abstract

Borneol, a monoterpenoid alcohol, is used widely, particularly in combined formulas for preventing and curing cardiovascular and cerebrovascular diseases in traditional Chinese medicine. In order to understand the blood and brain pharmacokinetics after intravenous, intranasal, or oral administration and to investigate the superiority and feasibility of intranasal administration, a simple gas chromatographic (GC) method with flame ionization detection (FID) was developed for the quantification of borneol. Blood samples and brain were collected from mice at 1, 3, 5, 10, 20, 30, 60, 90, and 120 min after intravenous, intranasal, or oral administration of borneol at a dosage of 30.0 mg/kg. Sample preparations were carried out by liquid-liquid extraction with an internal standard solution of octadecane. The pharmacokinetic parameters were calculated by the software of Kinetica. The calibration curves were linear in the range of 0.11-84.24 μg/ml and 0.16-63.18 μg/g for borneol in plasma and brain, respectively. The methodological and extraction recoveries were both in the range of 85%-115%. The intra-day and inter-day variabilities for plasma and brain samples were ≤5.00% relative standard deviation (RSD). The absolute bioavailabilities F of intranasal and oral administrations were 90.68% and 42.99%. The relative brain targeted coefficients Re of intranasal and oral administrations were 68.37% and 38.40%. The GC-FID method developed could be applied to determination and pharmacokinetic study. The borneol from injection was distributed and metabolized fast without absorption process. The borneol from oral administration was distributed more slowly and had the lowest absolute bioavailability. Nasal administration of borneol was quickly absorbed into the blood and brain, was easy to use and had a greater safety than infection, which makes it worthy of further development as an administration route for encephalopathy treatment.

In vivo microdialysis with ultra performance liquid chromatography–mass spectrometry for analysis of tetramethylpyrazine and its interaction with borneol in rat brain and blood

“…Thus, it can be seen that BO has a significant impact on the pharmacokinetic curves of TMP. In this study, BO markedly enhanced the brain and blood concentrations of TMP in the early stage within 2 h, which might be attributed to rapid metabolism of BO in vivo (Zhao et al, ). For many drugs, unbound drug concentrations in brain are much lower than the corresponding concentrations in plasma (Le Quellec, Dupin, Tufenkji, Genissel, & Houin, ), which was also supported in our results.…”

“…and BO (15 and 30 mg/kg, i.g. ; Yu, Ruan, Dong, et al, ; Zhao et al, ). In the pharmacodynamic experiment, rats ( n = 30) were randomly separated into five groups: a vehicle‐treated group; a sham‐operated group; a TMP group; a TMP + BO (15 mg/kg) group; and a TMP + BO (30 mg/kg) group.…”

Borneol, a novel agent that improves central nervous system drug delivery by enhancing blood–brain barrier permeability

“…The enhancing effects on the brain bioavailability of gastrodigenin, an active metabolite of gastrodin, reached a peak level with borneol doses of 200-600 mg/kg, but were attenuated with doses above 600 mg/kg (Cai et al, 2008). When borneol was given at different intervals, a robust enhancing effect on This table is modified based on Zhao et al (2012). Data are expressed as mean ± SD (n ¼ 5).…”

Surfactants and personal care products removal in pilot scale horizontal and vertical flow constructed wetlands while treating greywater

“…Temperatures of injector and detector were maintained at 250 and 280°C, respectively. Nitrogen was used as the carrier gas at flow rates of 1 mL/min, with a split ratio of 30:1 [30]. Standard graphs for PG and TMA were prepared individually by injecting known amounts of respective compound into a sealed reagent bottle equipped with Teflon septum.…”