Determination of mangiferin in rat eyes and pharmacokinetic study in plasma after oral administration of mangiferin-hydroxypropyl-beta-cyclodextrin inclusion.
OBJECTIVE
To determine whether mangiferin can enter the eye, because the eye possesses the unique blood-ocular barrier.


METHODS
Due to the low solubility of mangiferin, hydroxypropyl-beta-cyclodextrin was applied to improve the absorbance. A reversed-phase high-performance liquid chromatography assay for mangiferin in rat plasma and eye fluid was developed. The mobile phase consisted of methanol-0.6% glacial acetic acid (27:73, v/v) at a flow rate of 1.0 mL/min.


RESULTS
Peak areas of mangiferin were linear over a concentration range of 0.40-20.00 microg/mL in blood samples and a range of 0.10-5.00 microg/mL in eye samples, respectively. Intra- and interassay precision and accuracy of mangiferin fell well within the predefined limits of acceptability (<15%). The recovery was 81.12%-87.18% in the plasma and 79.96%-85.52% in the eye, respectively. The analytical method had excellent sensitivity using a small sample volume (20 microL) with the lower limit of quantification, 0.4 and 0.10 microg/mL for plasma and eye, respectively. Pharmacokinetic parameters of mangiferin in plasma were obtained as follows: T(max) = 7 h, C(max) = (4.43 +/- 0.62)microg/mL. The time point of 7 h was chosen for eye sample detection, as it had maximum plasma concentration. The concentration of mangiferin in the eye tissue 7 h after oral administration was (0.34 +/- 0.13)microg/mL (n = 6), coefficient of variation % = 38.24%.


CONCLUSIONS
Mangiferin can pass the blood-ocular barrier and is suitable to be used as an antioxidant in eye diseases.
Zhang
Hong
H
Eye Hospital, The First Affiliated Hospital, Harbin Medical University, Harbin, China.
Hou
Yunlong
Y
Liu
Yan
Y
Yu
Xuhui
X
Li
Baoxin
B
Cui
Hao
H
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000032:analysis / Q000493:pharmacokinetics*; D001813:Blood-Retinal Barrier; D002851:Chromatography, High Pressure Liquid; D005079:Excipients; D005123:Eye / Q000378:metabolism*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013535:Suspensions; D044004:Xanthones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D047392:beta-Cyclodextrins / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D000975:Antioxidants; D005079:Excipients; D013535:Suspensions; D044004:Xanthones; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C013592:mangiferin