Development of Novel Formulation Strategies to Improve Pharmacokinetic Profile of Resveratrol
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Resveratrol is a natural occurring polyphenol with diverse biological activities in vitro and poor pharmacokinetic profile because of its rapid metabolism in vivo. In this project, polymer conjugate approach was evaluated for masking resveratrol against the metabolism. Various polymer conjugates were prepared and evaluated both in vitro and in vivo. Among those tested, resveratrol-PLA-PEG and resveratrol-PEG ether conjugates were found capable of providing better pharmacokinetics than native resveratrol.
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Application of Solvent Influenced Fluorescence-quenching and Enhancement to Develop a Highly Sensitive HPLC Methodology for Analysis of Resveratrol-PEG ConjugatesBasavaraj, S; Benson, Heather; Brown, David; Chen, Yan (2013)Quantification of pegylated drugs in biological matrices is often complex and challenging. This paper describes a sensitive HPLC method with fluorescence detection for the analysis of pegylated resveratrol, resveratrol ...
Stabilization of resveratrol in blood circulation by conjugation to mPEG and mPEG-PLA polymers: Investigation of conjugate linker and polymer composition on stability, metabolism, antioxidant activity and pharmacokinetic profileSiddalingappa, B.; Benson, Heather; Brown, D.; Batty, Kevin; Chen, Y. (2015)Resveratrol is naturally occurring phytochemical with diverse biological activities such as chemoprevention, anti-inflammatory, anti-cancer, anti-oxidant. But undergoes rapid metabolism in the body (half life 0.13h). Hence ...
Development of a liquid chromatography/mass spectrometry methodology to separate, detect, characterize and quantify PEG-resveratrol prodrugs and the conjugation reaction precursors and intermediatesBasavaraj, S.; Benson, Heather; Cruickshank, C.; Brown, David; Chen, Yan (2011)A simple and reliable liquid chromatography/mass spectrometry (LC/MS) method to monitor pegylation of resveratrol is described. The developed LC/MS method can separate and quantify unmodified MeO-PEG-OH, carboxylic acid ...