betadex and mangiferin

The characterization, inclusion complexation behavior and binding ability of the inclusion complexes of mangiferin (MGF) with β-cyclodextrin and its derivatives (hydroxypropyl-β-cyclodextrin (HPβCD), sulfobutyl ether β-cyclodextrin (SBEβCD) and mono (6-ethylene-diamino-6-deoxy)-β-cyclodextrin (ENβCD)) were investigated in both solution and solid state by means of PL spectroscopy, (1)H and 2D NMR, XRD, TG and DSC. The results showed that the water solubility and thermal stability of MGF were significantly increased in the inclusion complex with cyclodextrins. The MGF/CDs complexes will be potentially useful for the design of a novel formulation of mangiferin for herbal medicine.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; beta-Cyclodextrins; Kinetics; Magnetic Resonance Spectroscopy; Powders; Solubility; Spectrometry, Fluorescence; Thermodynamics; Thermogravimetry; X-Ray Diffraction; Xanthones

The host-guest inclusion system of ethyl substituted β-cyclodextrin (DE-β-CD) with mangiferin (MA) was investigated by fluorescence spectra in solution. The results showed that the MA was encapsulated in the DE-β-CD's cavity to form a 2:1 stoichiometry host-guest inclusion complex (DE-β-CD/MA) and the inclusion constant (K=3.04×10(6)L(2)/mol(2)) was confirmed by the typical double reciprocal plots. Furthermore, several experimental conditions were optimized in order to obtain the maximum fluorescence signal. In addition, the thermodynamic parameters, Gibbs free energy (ΔG°), enthalpy change (ΔH°) and entropy change (ΔS°) of DE-β-CD/MA were obtained by the Van't Hoff equation. A spectrofluorimetric method for the determination of MA in solution in the presence of DE-β-CD was developed based on the remarkable enhancement of the fluorescence intensity of MA. The linear range was 2.00×10(-8)-7.00×10(-6)mol/L and the detection limit was 4.05×10(-9)mol/L. The proposed method was successfully applied to the analysis of MA in serum with the satisfactory result.

Topics: beta-Cyclodextrins; Humans; Hydrogen-Ion Concentration; Molecular Conformation; Spectrometry, Fluorescence; Thermodynamics; Xanthones

To determine whether mangiferin can enter the eye, because the eye possesses the unique blood-ocular barrier.. 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.. 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%.. Mangiferin can pass the blood-ocular barrier and is suitable to be used as an antioxidant in eye diseases.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Administration, Oral; Animals; Antioxidants; beta-Cyclodextrins; Blood-Retinal Barrier; Chromatography, High Pressure Liquid; Excipients; Eye; Male; Rats; Rats, Sprague-Dawley; Suspensions; Xanthones