title: Exploring the effect of Hesperetin-HSPC complex--a novel drug delivery system on the in vitro release, therapeutic efficacy and pharmacokinetics.
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.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Engineering and Technology, School of Natural Product Studies, Jadavpur University, Kolkata 700 032, India.
authors.forename: Kuntal
authors.initials: K
authors.lastname: Maiti
authors.forename: Kakali
authors.initials: K
authors.lastname: Mukherjee
authors.forename: Venkatesh
authors.initials: V
authors.lastname: Murugan
authors.forename: Bishnu Pada
authors.initials: BP
authors.lastname: Saha
authors.forename: Pulok Kumar
authors.initials: PK
authors.lastname: Mukherjee
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002138:Calibration; D002252:Carbon Tetrachloride Poisoning / Q000188:drug therapy / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D006569:Hesperidin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008111:Liver Function Tests; D008297:Male; D010713:Phosphatidylcholines / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012015:Reference Standards; D015203:Reproducibility of Results; D012995:Solubility; D013025:Glycine max / Q000737:chemistry; D013535:Suspensions
chemical_list: D000975:Antioxidants; D010713:Phosphatidylcholines; D013535:Suspensions; D006569:Hesperidin; C013015:hesperetin