Effect of different doses of borneol on the pharmacokinetics of vinpocetine in rat plasma and brain after intraocular administration

Abstract

1. The effect of different doses of borneol on the pharmacokinetics of vinpocetine after intraocular administration in the rat plasma and the brain was investigated.

2. Intraocular administration of vinpocetine (3 mg/kg) was performed, in combination with different doses (0, 5, 10, and 20 mg/kg) of borneol. Intravenous administration of vinpocetine was used as a control (1 mg/kg). The concentrations of vinpocetine in the rat plasma and the brain were determined using a liquid chromatography-tandem mass spectrometry (LC–MS/MS) method. Using the non-compartmental models with the DSA 2.0 software, the main pharmacokinetics parameters and the brain-targeting effect evaluated.

3. In comparison with intravenous administration, after intraocular administration of vinpocetine alone, the absolute bioavailability (F) of vinpocetine was 43.82% for the plasma, and the drug target index (DTI) was 1.05 for the brain. After intraocular administration of vinpocetine combined with different doses of borneol, the relative bioavailability (Fr) of vinpocetine in the plasma was increased by 130.46–182.90%. The relative bioavailability (Fr) of vinpocetine in the brain was improved (147.19–225.36%). The DTI was 1.12, 1.18, and 1.21 for 5, 10, and 20 mg/kg of borneol, respectively.

4. Compared with the intraocular administration of vinpocetine alone, the co-administration of different doses of borneol resulted in an obvious brain targeting effect.

Keywords:

• Vinpocetine
• borneol
• intraocular administration
• pharmacokinetics
• brain targeting effect
• LC–MS/MS

Disclosure statement

All the authors report that they have no conflict of interest.

Additional information

Funding

This work was supported by Natural Science foundation in higher education of Anhui Province (KJ2019A0454); Anhui Province “Special Support Plan” for the Second Batch of Innovative Leading Talents (The Second Batch).