Synthesis and Pharmacokinetics of Poly(Ethylene Glycol)-Modified Polysaccharide MDG-1 from Ophiopogon japonicus

JING Yn;LIN Xio;SHEN Ln;WNG Zhuo-jun;FENG Yi;XU De-sheng

Chinese Pharmaceutical Journal ›› 2010, Vol. 45 ›› Issue (18) : 1412-1416.

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PDF(1180 KB)
Chinese Pharmaceutical Journal ›› 2010, Vol. 45 ›› Issue (18) : 1412-1416.

Synthesis and Pharmacokinetics of Poly(Ethylene Glycol)-Modified Polysaccharide MDG-1 from Ophiopogon japonicus

  • JIANG Yan1,2, LIN Xiao1,3*, SHEN Lan3, WANG Zhuo-jun3, FENG Yi1, XU De-sheng4
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Abstract

OBJECTIVE To improve the pharmacokinetic properties of polysaccharide MDG-1 from Ophiopogon japonicus by modifying MDG-1 with polyethylene glycol (PEG). METHODS Linear amino-terminated poly(ethylene glycol) methyl ether was used to modify MDG-1. The apparent molecular weight and grafting degree of conjugates were determined by high-performance gel permeation chromatography (HPGPC). The pharmacokinetics of conjugates was investigated in rats. RESULTS Optimal modification conditions were obtained. Several conjugates with molecular-weight-different PEG and different grafting degree were prepared. The biological half-lives of the conjugates were significantly prolonged. And the prolongation was dependent not only on the molecular weight of PEG, but also on the grafting degree of the conjugates. CONCLUSION PEGylation is a promising method to improve pharmacokinetics of MDG-1.

Key words

Ophiopogon japonicus / polysaccharide / polyethylene glycol / pharmacokinetics / biological half-life

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JING Yn;LIN Xio;SHEN Ln;WNG Zhuo-jun;FENG Yi;XU De-sheng . Synthesis and Pharmacokinetics of Poly(Ethylene Glycol)-Modified Polysaccharide MDG-1 from Ophiopogon japonicus[J]. Chinese Pharmaceutical Journal, 2010, 45(18): 1412-1416

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