Poly(ethylene glycol)-radix Ophiopogonis polysaccharide conjugates: preparation, characterization, pharmacokinetics and in vitro bioactivity

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Xiao LinLan Shen

Abstract

Radix Ophiopogonis polysaccharide (ROP), a natural graminan-type fructan with Mw of ∼5kDa, had been found to have an excellent anti-myocardial ischemic activity. However, its rapid renal excretion following administration remarkably limits its efficacy and clinical use, which makes necessary the development of an effective delivery system. In this article, the feasibility of PEGylation to solve this problem was examined. A moderate coupling reaction between the hydroxyl-activated ROP and the amino-terminated mPEG was chosen to PEGylate ROP. Five different mPEG-ROP conjugates (with mPEG of molecular mass 2, 5 or 20kDa) were prepared, purified, characterized and evaluated in pharmacokinetics and in vitro bioactivity. Results showed that only when the apparent molecular weight of the conjugate approached to a certain value, would its plasma elimination reduce abruptly. In general, the conjugation caused the reduction in the bioactivity of ROP; however, well-preserved bioactivity was observed when the grafting degree of the conjugate was lower. Among the five conjugates studied, the one with an average 1.3 mPEG (20kDa) residues per single ROP was found to be satisfactory both in plasma retention and in bioactivity. It had a 47.4-fo...Continue Reading

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Citations

Jun 4, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·GuiLan SunYi Feng
Dec 2, 2011·International Journal of Nanomedicine·Xiao LinKe-Feng Ruan
Aug 17, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Robert HennigAchim Goepferich
Apr 25, 2012·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·GuiLan SunDeSheng Xu
Nov 4, 2015·International Journal of Biological Macromolecules·Yunpeng FanXiaoping Song
Jul 26, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Xiao LinDe-Sheng Xu
Dec 3, 2014·International Journal of Pharmaceutics·Yunpeng FanDewen Tong
Jul 20, 2016·International Journal of Biological Macromolecules·Qianqian DongYi Feng
Jan 10, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Azeguli HamutiJinyao Li
Dec 12, 2012·Journal of Separation Science·De-jun HuShao-ping Li
Jul 6, 2014·Beilstein Journal of Organic Chemistry·M Eugenia GiorgiRosa M de Lederkremer
Oct 10, 2021·International Journal of Pharmaceutics·Yanwei WangJingyan Wei

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