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Exploring the Effect of Hesperetin–HSPC Complex—A Novel Drug Delivery System on the In Vitro Release, Therapeutic Efficacy and Pharmacokinetics

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Abstract

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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Acknowledgments

This work was supported through the WOS-A grant [No. SR/WOS-A/LS-99/2007] of the Department of Science and Technology, Government of India, New Delhi to Dr. Kakali Mukherjee, for which the authors are grateful. Thanks are also due to the All India Council for Technical Education (AICTE), Government of India for providing financial assistance through MODROB research projects to the School of Natural Product Studies, Jadavpur University.

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Authors and Affiliations

  1. School of Natural Product Studies, Department of Pharmaceutical Technology, Faculty of Engineering and Technology, Jadavpur University, Kolkata, 700 032, India

    Kuntal Maiti, Kakali Mukherjee, Venkatesh Murugan, Bishnu Pada Saha & Pulok Kumar Mukherjee

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  1. Kuntal Maiti
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  2. Kakali Mukherjee
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  3. Venkatesh Murugan
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Correspondence to Pulok Kumar Mukherjee.

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Maiti, K., Mukherjee, K., Murugan, V. et al. Exploring the Effect of Hesperetin–HSPC Complex—A Novel Drug Delivery System on the In Vitro Release, Therapeutic Efficacy and Pharmacokinetics. AAPS PharmSciTech 10, 943–950 (2009). https://doi.org/10.1208/s12249-009-9282-6

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