BIO-POTENTIATION AND IN VIVO PHARMACOKINETICS STUDIES OF POLYPHENOLS FROM PUNICA GRANATUM BY FORMING PHOSPHOLIPID CONJUGATES FOR BETTER ANTIOXIDANT & ANTI-INFLAMMATORY ACTIVITY

Authors

  • Deep Bhattacharya Molecular Simulations Group, Department of Pharmaceutical Chemistry, Bombay College of Pharmacy, University of Mumbai, Kalina, Santacruz [East], Mumbai 400098. India.
  • Priscilla M D’mello Prin. K. M. Kundnani, College of Pharmacy
  • Tarun Kumar Dasgupta Prin. K. M. Kundnani, College of Pharmacy

Keywords:

Punica granatum, Flavonoids, In vivo, Glucuronide

Abstract

Objective: Polyphenols belong to the chemical class of flavonoids and are widely distributed in vegetables and plants. In this study, we aimed to potentiate the antioxidant and anti-inflammatory effects of polyphenols by forming a phospholipid complex of extracts from Punica granatum and also evaluating its in vivo pharmacokinetic parameters.

Methods: This method was used for determination and in vivo pharmacokinetics studies for the biomarkers and their lipid complexes from P. granatum extract. Anti-inflammatory and antioxidant studies ever performed on both uncomplexed and complexed flavonoids. Pharmacokineticbehaviour of biomarker was significantly improved with higher Cmax, t1/2 and shorter tmax& AUC0-t and AUC0-t values of glucuronide metabolites indicating the greater bioavailability.

Results: Anti lipid peroxidation inhibitory potential was found greater in case of phospholipid complexes with IC50 value 17.41 µg for biomarker complex as compared to biomarker mixture (63.52 µg) & anti-inflammatory activity of 100 mg/kg of agro waste extract complex of P. granatum was found very significant at 3rd hour with (21.95±0.071 %) inhibition in rat paw edema which was greater than the extract alone (11.13±0.084 %).

Conclusion: Bio-enhancement of polyphenols was observed and achieved through phospholipids complexes and was demonstrated by in vitro and in vivo activity testing by forming a supramolecular complex.

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Author Biography

Deep Bhattacharya, Molecular Simulations Group, Department of Pharmaceutical Chemistry, Bombay College of Pharmacy, University of Mumbai, Kalina, Santacruz [East], Mumbai 400098. India.

Molecular Simulations Group, Department of Pharmaceutical Chemistry, Bombay College of Pharmacy, University of Mumbai, Kalina, Santacruz [East], Mumbai 400098. India.

References

FA Bushra S, Muhammad R A, Shahzad ASC. Antioxidant potential of extracts from different age wastes. Grasas Y Ascites 2008;59:205-17.

GFPE Bombardelli. Complex compounds of bioflavonoid with phospholipids, their preparation and use, and pharmaceutical and cosmetic compositions containing them; 1991.

KMAYK, Junji T. Conjugated quercetin glucuronides as bioactive metabolites and precursors of aglycone in vivo. Food Funct 2011;11:11-7.

QPYOC Xiao, Z Zhong, SSC Moses. Pharmacokinetics and modelling of Quercetin and metabolites. Am Assoc Pharm Sci 1992;9:350-6.

ON Ohkawa, HK Yagi. Assay for lipid peroxides in animal tissues by phenobarbitone acid reaction. Anal Biochem 1979;95:351–8.

ZP Zhenbin Wang, Haile Ma, Griffiths G. Atungulu. Extract of phenolicsfrom pomegranate peels. Open Food Sci J 2011;5:17-25.

NM Pandey, SI Rizvi. Protective role of myricetin on markers of oxidative stress in human erythrocytes subjected to oxidative stress. Nat Prod Commun 2009;4:221–6.

REANGW, Winter CA. Carrageenan induced edema in hind paw of the rat as an assay for anti-inflammatory drugs. Proc Soc Exp Biol Med 1962;111:544-7.

BA Khanduja KL. Stable free radical scavenging and antiperoxidative properties of resveratrol compared in vitro with some other bioflavonoid. Indian J Biochem Biophys 2003;40:416-22.

DSC Sarkar M, Saha SK, Mahmud ZA, SC Das, SC Bachar. Analgesic and anti-inflammatory activities of flower extracts of Punica granatum. J Appl Pharm Sci 2012;2:133-6.

S-LH, Chi-Yu Y, Kuo-Ching W, Shiuan-Pey L, Shang-yuantsai, Yu-chi hou, et al. Bioavailability and metabolic pharmacokinetics of Rutin and Quercetin in rats. J Food Drug Anal 2005;13:244-50.

X.-N L, Xie L, Jiang D, Zhang D. Determination and pharmacokinetics study of catechin in rat plasma by HPLC. J Pharm Anal 2011;1:297–301.

MK Murugan V, Maiti K, Mukherjee PK. Enhanced oral bioavailability and antioxidant profile of telluric acid in phospholipids. J Agric Food Chem 2009;57:4559-65.

MK Maiti K, Gantait A, Saha B, Mukherjee PK. Enhanced therapeutic potential of naringeninâ€phospholipid complex in rats. J Pharm Pharmacol 2006;58:1227â€33.

Published

01-03-2015

How to Cite

Bhattacharya, D., P. M. D’mello, and T. K. Dasgupta. “BIO-POTENTIATION AND IN VIVO PHARMACOKINETICS STUDIES OF POLYPHENOLS FROM PUNICA GRANATUM BY FORMING PHOSPHOLIPID CONJUGATES FOR BETTER ANTIOXIDANT & ANTI-INFLAMMATORY ACTIVITY”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 3, Mar. 2015, pp. 164-72, https://innovareacademics.in/journals/index.php/ijpps/article/view/4117.

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