Ellagic acid (EA) has been reported as a potent antioxidant from natural resources with several nutritional benefits. The major disadvantage of this phytoconstituent is its rapid elimination from the body after administration. To overcome this limitation, a novel dietary formulation of EA with phospholipid was developed to investigate the effect of this complex on carbon tetrachloride induced liver damage in rats. The antioxidant activity of the complex (equivalent of EA = 25 and 50 mg/kg of body weight) and free EA (25 and 50 mg/kg of body weight) was evaluated by measuring various enzymes in oxidative stress condition. The complex significantly protected the liver by restoring the activity of superoxide dismutase, catalase and liver glutathione, and thiobarbituric acid reactive substances with respect to the carbon tetrachloride treated group (P < 0.05 and < 0.01). The complex provided better protection to rat liver than free EA at the same dose. The serum concentration of EA obtained from the complex (equivalent to 80 mg/kg of EA) was higher (C(max) = 0.54 microg/mL) than that of pure EA (80 mg/kg) (C(max) = 0.21 microg/mL), and the complex maintained effective concentration for a longer period of time in serum. The experimental outcome highlighted better hepatoprotective activity of the EA complex due to its potential antioxidant property compared with the free EA tested at the same dose level.

The results proved that the andrographolide complex produced by this method has better bioavailability and hence improved hepatoprotective activity compared with andrographolide at the same dose. Andrographolide complexation is therefore helpful in solving the problem of rapid clearance and low elimination half-life associated with andrographolide from A. paniculata.

Hesperetin is known to exhibit a variety of pharmacological activities in mammalian cell systems. Although it shows appreciable bioavailability when administered orally, its faster elimination from body creates the need of frequent administration to maintain effective plasma concentration. To overcome this limitation, a phospholipid complex of hesperetin was prepared and evaluated for antioxidant activity and pharmacokinetic profile. The hesperetin content of the complex was determined by a spectrophotometer and the surface characteristics of the complex were studied by means of microscope. The antioxidant activity was evaluated in carbon-tetrachloride-intoxicated rats at a dose level of 100 mg/kg body weight, p.o. The complex was studied for in vitro drug release characteristics and effect of complexation on serum concentration of hesperetin in rats was also studied along with main pharmacokinetic parameters. The results showed that the complex has a sustained release property and enhanced antioxidant activity (P < 0.05 and <0.01) as compared to free hesperetin at the same dose level. Pharmacokinetic study depicted that the complex has higher relative bioavailability and acted for a longer period of time. The study therefore suggests that phospholipid complex of hesperetin produced better antioxidant activity than free drug at the same dose level and the effect persisted for a longer period of time, which may be helpful in solving the problems of faster elimination of the molecule.

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The hydroalcoholic extract of fruit pulp of Terminalia chebula Retz. was standardized and evaluated for its safety through cytochrome P450 (CYP 450) inhibition assay. Standardization was performed through high performance thin layer chromatography (HPTLC) using gallic acid (GA) standard. Cytochrome P450-CO complex microplate assay was performed using rat liver microsomes. The effect of standardized extract, its fraction and bioactive marker compound were comparatively evaluated for its effect on CYP P450 enzymes. The extract of fruit pulp was used for HPTLC, where the R(f) value of the marker was found to be 0.43. The calibration plot was linear in the range of 2-14 µg of GA and correlation co-efficient of 0.99965. The mean quantity of GA was found to be 2.5% w/w. The CYP P450 concentration of the rat liver microsome sample used in the study was found to be 0.417 nmol/mg protein. The in vitro effect of various concentrations of extracts and fractions showed a linear concentration-dependent inhibition of cytochrome P450 up to 60 µL. The study showed more inhibition of fraction when compared to the extract and GA. Still, the inhibition showed by fraction is less when compared with standard Ketoconazole. Thus, this study indicated the in vitro cytochrome P450 inhibition potential of T. Chebula.