Pharmacokinetic study of mangiferin in rat plasma and retina using high-performance liquid chromatography.
OBJECTIVE
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.
Hou
Yunlong
Y
Department of Pharmacology, Harbin Medical University, Harbin, PR China.
Fan
Shengjun
S
Zhang
Hong
H
Gu
Yuanqin
Y
Yu
Xuhui
X
Li
Baoxin
B
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012160:Retina / Q000378:metabolism; D044004:Xanthones / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*
D044004:Xanthones; C013592:mangiferin
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