Enhancement of bioavailability of phytomolecules with value added formulation

Hesperetin is a potent phytomolecule with several therapeutic benefits including antioxidant, lipid-lowering, anti-carcinogenic activities. But its short half-life and rapid clearance from the body restricts its use [1]. To overcome this limitation, a novel hesperetin-phospholipid complex was developed. The complex was prepared with hesperetin and hydrogenated soy phosphatidyl-choline at a molar ratio of 1:1 as reported [2, 3]. The prepared complexes were characterized by organoleptic examination, UV-, IR-, NMR-, DSC-characterization. The complex was tested for its antioxidant activity in CCl₄-intoxicated rats in comparison to the parent molecule. Further studies were performed to evaluate the pharmacokinetic parameters of the complex and hesperetin in rats. The antioxidant activity was evaluated at a dose level of 100mg/kg body weight, p.o. The complex was studied for in- vitro drug release properties and the effect of complexation on serum concentration and pharmacokinetics was studied by HPLC. The complex showed sustained release relase of hesperetin for over 24 hours and enhanced antioxidant activity (P<0.05 and <0.01) as compared to free hesperetin at the same dose level. Pharmacokinetic studies depicted that the complex has higher relative bioavailability than the pure phytomolecule. The results suggest that a phospholipid complex of hesperetin results in better antioxidant activity than free hesperetin at the same dose level and that the effect persisted for a longer period of time, which may be helpful in solving the problems of too fast elimination of the molecule.

Acknowledgements: Department of Science and Technology, Ministry of Science and Technology, Government of India, New Delhi for necessary financial assistance for this work.

References: 1. Erlund, et al. (2001)J. Nutr. 131: 235–241.

2. Maiti, K. et al. (2007) Int. J. Pharmaceutics 330: 155–163.

3. Maiti, K. et al. (2006)J. Pharm. Pharmacol. 9: 1227–1233.