Poly (ethylene glycol) prodrug for puerarin and its characteristic evaluation

A puerarin prodrug was prepared pharmaceutically by covalently linking puerarin to a drug carrier monomethoxypolyethylene glycol (mPEG, MW=2000Da ) via a glycine (Gly) spacer. And the products were validated by UV, FI-IR and ¹H NMR. We evaluated the hemolytic property of the prodrug, the results showed that it produced minimal hematotoxicity as often shown by puerarin injectible. And the protective effect of prodrug on acute myocardial ischemia model implied better therapeutic effect than puerarin injectible. Our data suggest that the puerarin PEG conjugation is a promising prodrug that exhibits better aqueous solubility, much less side effects and more effective than puerarin.