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

Author

Jin, Bo ; Jiang, Fusheng ; Liu, Xia ; Yu, Meirong ; Ding, Zhishan

Author_Institution

Coll. of Life & Sci., Zhejiang Chinese Med. Univ., Hangzhou, China

fYear

2011

fDate

24-26 June 2011

Firstpage

7718

Lastpage

7721

Abstract

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.

Keywords

Fourier transform spectra; biochemistry; biological NMR; blood; cardiology; drugs; infrared spectra; organic compounds; spectrochemical analysis; toxicology; ultraviolet spectra; ¹H NMR; FT-IR technique; UV technique; acute myocardial ischemia model; aqueous solubility; covalent linking; drug carrier; glycine spacer; hematotoxicity; hemolytic property; monomethoxypolyethylene glycol; pharmaceutical preparation; poly (ethylene glycol) prodrug; puerarin PEG conjugation; puerarin injectible; side effects; therapeutic effect; Diseases; Drugs; Mice; Nuclear magnetic resonance; Polymers; Solvents; Hemotoxicity; PEGylation; Pharmacodynamics; Prodrugs; Puerarin;

fLanguage

English

Publisher

ieee

Conference_Titel

Remote Sensing, Environment and Transportation Engineering (RSETE), 2011 International Conference on

Conference_Location

Nanjing

Print_ISBN

978-1-4244-9172-8

Type

conf

DOI

10.1109/RSETE.2011.5966164

Filename

5966164