Pharmacokinetic study of mangiferin in rat plasma and retina using high-performance liquid chromatography

[摘要] Purpose: Although the naturallyoccurring antioxidant mangiferin has been widely used, it is not yetknown whether it can cross the blood-retina barrier (BRB) and enter theeye. The purpose of this experiment was to investigate the ability ofmangiferin to pass the blood-retina barrier. Methods: Sprague–Dawley rats were usedfor biologic fluid sampling after intravenous administration ofmangiferin at doses of 10, 25, and 50 mg/kg. Blood and retina sampleswere collected at different time points post-dose. High-performanceliquid chromatography (HPLC) separation was conducted on a COSMOSIL 5C18—MS—IIcolumn(4.6mm×250mm, 5 μm) with a flow rate of 1.0 ml/min using amobile phase comprised of methanol −2% glacial acetic acid (40:60 v:v).Results: The HPLC method has provensuitable to determine the presence of mangiferin in the eye. The plasmaconcentration of mangiferin was dose dependent. Pharmacokineticparameters of mangiferin in plasma after intravenous administrationwere fitted to the two-compartment model with the first-orderelimination and first-order transfer between central and peripheralcompartments. The concentration of mangiferin in the retina goes withthat in the blood. Mangiferin concentrations in the retina reached5.69±1.48 μg/ml 0.5 h after intravenous administration (50 mg/kg) andthen dropped gradually to 0.30±0.02 μg/ml 5.0 h later. Theeye–to-plasma concentration ratio was 2.80%. Conclusions: Mangiferin can pass theblood-retina barrier after a single intravenous administration and maybe a potential natural antioxidant in treating eye diseases.

[学科分类] 生物化学/生物物理