BACKGROUND: Andrographis paniculata is a health food used extensively in Southeast Asia, India and China and contains the pharmacologically important phytochemical andrographolide. Although andrographolide has antihepatotoxic activity, its bioavailability from A. paniculata is restricted by its rapid clearance and high plasma protein binding. The aim of this study was to formulate a herbosome of andrographolide with a naturally occurring phospholipid in order to enhance the bioavailability and hepatoprotective activity of andrographolide in rats. RESULTS: Andrographolide herbosome equivalent to 25 and 50 mg kg(-1) andrographolide significantly protected the liver of rats, restoring hepatic enzyme activities with respect to carbon tetrachloride-treated animals (P < 0.05 and P < 0.01 respectively). The rat plasma concentration of andrographolide obtained from the complex equivalent to 25 mg kg(-1) andrographolide (C(max) = 9.64 microg mL(-1)) was higher than that obtained from 25 mg kg(-1) andrographolide (C(max) = 6.79 microg mL(-1)), and the complex maintained its effective plasma concentration for a longer period of time. CONCLUSION: The results proved that the andrographolide complex produced by this method has better bioavailability and hence improved hepatoprotective activity compared with andrographolide at the same dose. Andrographolide complexation is therefore helpful in solving the problem of rapid clearance and low elimination half-life associated with andrographolide from A. paniculata. Copyright (c) 2009 Society of Chemical Industry.
BACKGROUND:Andrographis paniculata is a health food used extensively in Southeast Asia, India and China and contains the pharmacologically important phytochemical andrographolide. Although andrographolide has antihepatotoxic activity, its bioavailability from A. paniculata is restricted by its rapid clearance and high plasma protein binding. The aim of this study was to formulate a herbosome of andrographolide with a naturally occurring phospholipid in order to enhance the bioavailability and hepatoprotective activity of andrographolide in rats. RESULTS:Andrographolide herbosome equivalent to 25 and 50 mg kg(-1) andrographolide significantly protected the liver of rats, restoring hepatic enzyme activities with respect to carbon tetrachloride-treated animals (P < 0.05 and P < 0.01 respectively). The rat plasma concentration of andrographolide obtained from the complex equivalent to 25 mg kg(-1) andrographolide (C(max) = 9.64 microg mL(-1)) was higher than that obtained from 25 mg kg(-1) andrographolide (C(max) = 6.79 microg mL(-1)), and the complex maintained its effective plasma concentration for a longer period of time. CONCLUSION: The results proved that the andrographolide complex produced by this method has better bioavailability and hence improved hepatoprotective activity compared with andrographolide at the same dose. Andrographolide complexation is therefore helpful in solving the problem of rapid clearance and low elimination half-life associated with andrographolide from A. paniculata. Copyright (c) 2009 Society of Chemical Industry.