INVIVO FATE OF END-CHAIN RADIOLABELED POLY(BETA-MALIC ACID), A WATER-SOLUBLE BIODEGRADABLE DRUG CARRIER

被引:23
作者
FOURNIE, P [1 ]
DOMURADO, D [1 ]
GUERIN, P [1 ]
BRAUD, C [1 ]
VERT, M [1 ]
MADELMONT, JC [1 ]
机构
[1] UNIV COMPIEGNE,TECHNOL ENZYMAT LAB,CNRS,URA 523,BP 649,F-60206 COMPIEGNE,FRANCE
关键词
D O I
10.1177/088391159000500401
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
In a first attempt to determine the fate of poly(beta-malic acid) after intravenous injection in mice, polymer end-chain C-14-radiolabelling was achieved using C-14-treithylamine as the initiator for the ring-opening polymerization of benzyl malolactonate. The corresponding poly(beta-malic acid) sodium salt (M(w) approximately 30,000) exhibited an activity of 4.2-mu-Ci.g-1. Aliguots of a neutral isoosmotic solution of the latter were given intravenously to mice through a lateral tail vein. Radioactivity was counted in the liver, kidney, intestine, lung, brain, spleen, heart, muscle, urine and blood for various post-injection times up to 24 hours. Fast urinary excretion (70% after 1 hour and 90% after 6 hours) was observed. For all the sites investigated, radioactivity decreased exponentially except in the liver and kidneys were a small peak was detected after 2 hours. Further investigations with ploy(beta-malic acid) radiolabelled in repeating units will be necessary to overcome the shortcomings of the end-chain radiolabelling method applied to degradable polymers.
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页码:381 / 395
页数:15
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