Impact of the Herbal Breviscapine on the Pharmacokinetics of Simvastatin in Rats: The Involvement of CYP3A4

Ju, Aixia; Li, Yang Yang; Qu, Zhe; Li, Qiuhong

doi:10.1055/s-0042-118170

Cited by 9 publications

(8 citation statements)

References 13 publications

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“…Rats in the TBI + BVP and TBI + vehicle groups were administrated BVP intraperitoneally (50 mg/kg body weight) or equal volumes of DMSO, respectively, 30 minutes after TBI. Drug doses used in the study were used according to the previous study …”

Section: Methodsmentioning

confidence: 99%

Breviscapine provides a neuroprotective effect after traumatic brain injury by modulating the Nrf2 signaling pathway

Wang

Zhang

et al. 2019

J of Cellular Biochemistry

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Breviscapine (BVP) has been widely used in the treatment of several systemic diseases, including those of the cardiovascular and cerebrovascular systems. But, few studies have looked at the neuroprotective effects of BVP and its potential effect in treating traumatic brain injury (TBI). The present study investigated the neuroprotective effect of BVP following TBI and illuminated the underlying mechanism. The weight drop‐induced closed diffuse traumatic brain injury method was used to induce TBI in rats. BVP was injected intraperitoneally 30 minutes after TBI. Neurologic scores were performed to measure behavioral outcomes. Nissl staining and terminal deoxynucleotidyl transferase‐mediated dUTP nick‐end labeling (TUNEL) assays were performed on histopathologic tissue sections to evaluate neuronal apoptosis. The nuclear factor erythroid 2‐related factor 2 (Nrf2) and its related downstream proteins, including heme oxygenase‐1 (HO‐1) and quinine oxidoreductase‐1 (NQO1) were detected with Western blots. BVP treatment alleviated or attenuated TBI‐induced neuron cell apoptosis and improved neurobehavioral functions through the upregulated expression of Nrf2 and its related downstream proteins. This study, using the drug, BVP, we present new mechanisms responsible for neuronal apoptosis in TBI with possible involvement of the Nrf2 pathway.

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Section: Methodsmentioning

confidence: 99%

Breviscapine provides a neuroprotective effect after traumatic brain injury by modulating the Nrf2 signaling pathway

Wang

Zhang

et al. 2019

J of Cellular Biochemistry

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“…However, despite these pharmacological functions, BRE also has some disadvantageous characteristics such as low aqueous solubility, poor chemical stability, short biological half-life and unsatisfactory bioavailability, which greatly limit its clinical application. 5,6 Therefore, it is necessary to develop a formulation that can overcome the above shortcomings.…”

Section: Introductionmentioning

confidence: 99%

<p>Improving Solubility and Bioavailability of Breviscapine with Mesoporous Silica Nanoparticles Prepared Using Ultrasound-Assisted Solution-Enhanced Dispersion by Supercritical Fluids Method</p>

Yang

et al. 2020

IJN

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Background: Breviscapine (BRE) has significant efficacy in cardiovascular disease, but the poor water solubility of breviscapine affects its oral absorption and limits its clinical application. In this study, supercritical carbon dioxide (SCF-CO 2) technology was used to improve the solubility and bioavailability of BRE loaded into mesoporous silica nanoparticles (MSNs). Methods: The solubility of BRE in SCF-CO 2 was measured under various conditions to investigate the feasibility of preparing drug-loaded MSNs by using ultrasound-assisted solution-enhanced dispersion by supercritical fluids (USEDS). The preparation process of drugloaded MSNs was optimized using the central composite design (CCD), and the optimized preparation was comprehensively characterized. Furthermore, the drug-loaded MSNs prepared by the conventional method were compared. Finally, the dissolution and bioavailability of the preparations were evaluated by in vitro release and pharmacokinetics study. Results: The solubility of BRE in SCF-CO 2 was extremely low which was suitable to prepare BRE-loaded MSNs by USEDS technology. The particle size of the preparation was 177.24 nm, the drug loading was 8.63%, and the specific surface area was 456.3m 2 /g. As compared to the conventional preparation method of solution impregnation-evaporation (SIV), the formulation prepared by USEDS technology has smaller particle size, higher drug loading, less residual solvent and better stability. The results of the in vitro release study showed that drug-loaded MSNs could significantly improve drug dissolution. The results of pharmacokinetics showed that the bioavailability of drug-loaded MSNs was increased 1.96 times compared to that of the BRE powder. Conclusion: Drug-loaded MSNs can significantly improve the solubility and bioavailability of BRE, indicating a good application prospect for MSNs in improving the oral absorption of drugs. In addition, as a solid dispersion preparation technology, USEDS technology has incomparable advantages.

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“…In a previous study, the combination of simvastatin and berviscapine increased the plasma concentration of simvastatin by inhibiting the mRNA expression of the hepatic CYP3A4 (Ju et al. 2017 ).…”

Section: Introductionmentioning

confidence: 96%

“…The pharmacokinetics of simvastatin that depends on its metabolism and absorption is the main factor that affected the curative effectiveness (Jiang et al 2017). In a previous study, the combination of simvastatin and berviscapine increased the plasma concentration of simvastatin by inhibiting the mRNA expression of the hepatic CYP3A4 (Ju et al 2017).…”

Section: Introductionmentioning

confidence: 99%

Baicalein inhibits the pharmacokinetics of simvastatin in rats via regulating the activity of CYP3A4

Meng

Zhang

et al. 2021

Pharmaceutical Biology

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Context: Baicalein and simvastatin possess similar pharmacological activities and indications. The risk of their co-administration was unclear. Objective: The interaction between baicalein and simvastatin was investigated to provide reference and guidance for the clinical application of the combination of these two drugs. Materials and methods: The pharmacokinetics of simvastatin was investigated in Sprague-Dawley rats (n ¼ 6). The rats were pre-treated with 20 mg/kg baicalein for 10 days and then administrated with 40 mg/ kg simvastatin. The single administration of simvastatin was set as the control group. The rat liver microsomes were employed to assess the metabolic stability and the effect of baicalein on the activity of CYP3A4. Results: Baicalein significantly increased the AUC (0-t) (2018.58 ± 483.11 vs. 653.05 ± 160.10 lg/L Â h) and C max (173.69 ± 35.49 vs. 85.63 ± 13.28 lg/L) of simvastatin. The t 1/2 of simvastatin was prolonged by baicalein in vivo and in vitro. The metabolic stability of simvastatin was also improved by the co-administration of baicalein. Baicalein showed an inhibitory effect on the activity of CYP3A4 with the IC 50 value of 12.03 lM, which is responsible for the metabolism of simvastatin. Discussion and conclusion: The co-administration of baicalein and simvastatin may induce drug-drug interaction through inhibiting CYP3A4. The dose of baicalein and simvastatin should be adjusted when they are co-administrated.

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Impact of the Herbal Breviscapine on the Pharmacokinetics of Simvastatin in Rats: The Involvement of CYP3A4

Cited by 9 publications

References 13 publications

Breviscapine provides a neuroprotective effect after traumatic brain injury by modulating the Nrf2 signaling pathway

Breviscapine provides a neuroprotective effect after traumatic brain injury by modulating the Nrf2 signaling pathway

<p>Improving Solubility and Bioavailability of Breviscapine with Mesoporous Silica Nanoparticles Prepared Using Ultrasound-Assisted Solution-Enhanced Dispersion by Supercritical Fluids Method</p>

Baicalein inhibits the pharmacokinetics of simvastatin in rats via regulating the activity of CYP3A4

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