Herbosomes enhances in vivo antioxidant activity of Punica granatum extracts

Background: Punica granatum (Pomegranates) show excellent anti-oxidant activity in vitro and Punicalagins, pair of ellagitannins present in pomegranates are considered to be responsible for the same. Punicalagins are poorly absorbed from GIT. Poor lipophilicity limit their ability to cross the bilipid layer of GIT. Punicalagins also get degraded by colonic microflora to generate molecules of ellagic acid and these molecules have poor solubility in the GI fluid. Hence, Punicalagins which show excellent in vitro antioxidant activity fail to depict the same in vivo. In the present research project, a novel delivery system, herbosomes, is developed with a view to enhance the antioxidant activity of pomegranate extract in vivo.

Methods: Herbosomes were developed by mixing standardized pomegranate extracts with phospholipids in 1:1 mixture of dioxane and methanol followed by spray drying. The herbosomes were obtained in powder form which was characterized by Infrared spectroscopy, SEM, DSC, and XRD study.

Standardized pomegranate extracts and herbosomes of the same were evaluated for antioxidant activity by estimation of SOD, catalase, glutathione peroxidase and glutathione reductase enzymes in CCl4 induced hepatotoxicity animal model.

Result: Different characterization studies confirmed complexation between the phospholipid and active constituents of the extracts. Herbosomes at the dose of 100 mg/kg showed significant in vivo antioxidant activity as compared to same dose of the pomegranate extracts. This effect was evident by restoration of the antioxidant enzymes to the normal level in carbon tetrachloride induced hepatotoxicity.

Conclusion: There are many bioactive phytoconstituents which show excellent pharmacological activity in vitro, but fail to show the same in vivo because of limited permeability through biological membrane or gut degradation. Formation of herbosomes i.e complexation with phospholipids can be effective technique to overcome this problem.

Keywords: Herbosomes, punica granatum, punicalagins

References:

[1] Seeram, N.P. et al, In vitro antiproliferative, apoptotic and antioxidant activities of punicalagin, ellagic acid and a total pomegranate tannin extract are enhanced in combination with other polyphenols as found in pomegranate juice, The Journal of Nutritional Biochemistry, 2005 Jun;16(6): 360 – 7

[2] Cedra B et al. Evaluation of the bioavailability and metabolism in the rat of punicalagin, an antioxidant polyphenol from pomegranate juice, European Journal of Nutrition, 2003 Jan;42(1): 18 – 28.