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

Hou Y, Fan S, Zhang H, Gu Y, Yu X, Li B - Mol. Vis. (2010)

Bottom Line: Mangiferin concentrations in the retina reached 5.69+/-1.48 microg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30+/-0.02 microg/ml 5.0 h later.The eye-to-plasma concentration ratio was 2.80%.Mangiferin can pass the blood-retina barrier after a single intravenous administration and may be a potential natural antioxidant in treating eye diseases.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, Harbin Medical University, Harbin, PR China.

ABSTRACT

Purpose: Although the naturally occurring antioxidant mangiferin has been widely used, it is not yet known whether it can cross the blood-retina barrier (BRB) and enter the eye. The purpose of this experiment was to investigate the ability of mangiferin to pass the blood-retina barrier.

Methods: Sprague-Dawley rats were used for biologic fluid sampling after intravenous administration of mangiferin at doses of 10, 25, and 50 mg/kg. Blood and retina samples were collected at different time points post-dose. High-performance liquid chromatography (HPLC) separation was conducted on a COSMOSIL 5C(18)-MS-II column (4.6 mm x 250 mm, 5 microm) with a flow rate of 1.0 ml/min using a mobile phase comprised of methanol -2% glacial acetic acid (40:60 v:v).

Results: The HPLC method has proven suitable to determine the presence of mangiferin in the eye. The plasma concentration of mangiferin was dose dependent. Pharmacokinetic parameters of mangiferin in plasma after intravenous administration were fitted to the two-compartment model with the first-order elimination and first-order transfer between central and peripheral compartments. The concentration of mangiferin in the retina goes with that in the blood. Mangiferin concentrations in the retina reached 5.69+/-1.48 microg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30+/-0.02 microg/ml 5.0 h later. The eye-to-plasma concentration ratio was 2.80%.

Conclusions: Mangiferin can pass the blood-retina barrier after a single intravenous administration and may be a potential natural antioxidant in treating eye diseases.

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Related in: MedlinePlus

Mean level of mangiferin in rat blood after mangiferin administration (10, 25, and 50 mg/kg, i.v.). Data are expressed as mean±SEM (n=6). The concentration-time data after a single intravenous administration of 10, 25, or 50 mg/kg showed that the major parameters were correlated positively with the dosage given. The mean plasma concentration–time profile is illustrated here.
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f4: Mean level of mangiferin in rat blood after mangiferin administration (10, 25, and 50 mg/kg, i.v.). Data are expressed as mean±SEM (n=6). The concentration-time data after a single intravenous administration of 10, 25, or 50 mg/kg showed that the major parameters were correlated positively with the dosage given. The mean plasma concentration–time profile is illustrated here.

Mentions: The sampling technique and liquid chromatographic detection were then applied to the pharmacokinetic characterization using the DAS 2.0 program (Drug and Statistics 2.0, Hefei, China). After a single intravenous administration of 10, 25, or 50 mg/kg of mangiferin, the concentration-time data conformed to a two-compartment model and the major parameters correlated positively with the dosage given. The dosages for Cmax were 24.75±0.85, 56.77±21.13, and 200.77±32.12 μg/ml, respectively, for AUC(0-t), they were 121.48±12.92, 205.28±104.30, and 577.71±63.30l μg/ml/h, respectively. The pharmacokinetic parameters are listed in Table 4. The mean plasma concentration–time profile is illustrated in Figure 4. Results of the study are consistent with the works by Lai [17] and with other previously published studies [12–16]. Detectable mangiferin was found in the eye, as shown in Table 5.The mangiferin concentration reached 5.69±1.48 μg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30±0.02 μg/ml 5.0h later. The pharmacokinetic parameters of the retina are listed in Table 6.


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

Hou Y, Fan S, Zhang H, Gu Y, Yu X, Li B - Mol. Vis. (2010)

Mean level of mangiferin in rat blood after mangiferin administration (10, 25, and 50 mg/kg, i.v.). Data are expressed as mean±SEM (n=6). The concentration-time data after a single intravenous administration of 10, 25, or 50 mg/kg showed that the major parameters were correlated positively with the dosage given. The mean plasma concentration–time profile is illustrated here.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2927378&req=5

f4: Mean level of mangiferin in rat blood after mangiferin administration (10, 25, and 50 mg/kg, i.v.). Data are expressed as mean±SEM (n=6). The concentration-time data after a single intravenous administration of 10, 25, or 50 mg/kg showed that the major parameters were correlated positively with the dosage given. The mean plasma concentration–time profile is illustrated here.
Mentions: The sampling technique and liquid chromatographic detection were then applied to the pharmacokinetic characterization using the DAS 2.0 program (Drug and Statistics 2.0, Hefei, China). After a single intravenous administration of 10, 25, or 50 mg/kg of mangiferin, the concentration-time data conformed to a two-compartment model and the major parameters correlated positively with the dosage given. The dosages for Cmax were 24.75±0.85, 56.77±21.13, and 200.77±32.12 μg/ml, respectively, for AUC(0-t), they were 121.48±12.92, 205.28±104.30, and 577.71±63.30l μg/ml/h, respectively. The pharmacokinetic parameters are listed in Table 4. The mean plasma concentration–time profile is illustrated in Figure 4. Results of the study are consistent with the works by Lai [17] and with other previously published studies [12–16]. Detectable mangiferin was found in the eye, as shown in Table 5.The mangiferin concentration reached 5.69±1.48 μg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30±0.02 μg/ml 5.0h later. The pharmacokinetic parameters of the retina are listed in Table 6.

Bottom Line: Mangiferin concentrations in the retina reached 5.69+/-1.48 microg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30+/-0.02 microg/ml 5.0 h later.The eye-to-plasma concentration ratio was 2.80%.Mangiferin can pass the blood-retina barrier after a single intravenous administration and may be a potential natural antioxidant in treating eye diseases.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, Harbin Medical University, Harbin, PR China.

ABSTRACT

Purpose: Although the naturally occurring antioxidant mangiferin has been widely used, it is not yet known whether it can cross the blood-retina barrier (BRB) and enter the eye. The purpose of this experiment was to investigate the ability of mangiferin to pass the blood-retina barrier.

Methods: Sprague-Dawley rats were used for biologic fluid sampling after intravenous administration of mangiferin at doses of 10, 25, and 50 mg/kg. Blood and retina samples were collected at different time points post-dose. High-performance liquid chromatography (HPLC) separation was conducted on a COSMOSIL 5C(18)-MS-II column (4.6 mm x 250 mm, 5 microm) with a flow rate of 1.0 ml/min using a mobile phase comprised of methanol -2% glacial acetic acid (40:60 v:v).

Results: The HPLC method has proven suitable to determine the presence of mangiferin in the eye. The plasma concentration of mangiferin was dose dependent. Pharmacokinetic parameters of mangiferin in plasma after intravenous administration were fitted to the two-compartment model with the first-order elimination and first-order transfer between central and peripheral compartments. The concentration of mangiferin in the retina goes with that in the blood. Mangiferin concentrations in the retina reached 5.69+/-1.48 microg/ml 0.5 h after intravenous administration (50 mg/kg) and then dropped gradually to 0.30+/-0.02 microg/ml 5.0 h later. The eye-to-plasma concentration ratio was 2.80%.

Conclusions: Mangiferin can pass the blood-retina barrier after a single intravenous administration and may be a potential natural antioxidant in treating eye diseases.

Show MeSH
Related in: MedlinePlus