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In Vivo Fate of End-Chain Radiolabelled Poly(ß-malic acid), a Water-Soluble Biodegradable Drug Carrier

Laboratoire de Technologie Enzymatique U.R.A. n° 523 du C.N.R.S. Université de Compiègne BP 649, 60206 Compiègne Cedex, France

Dominique Domurado

Laboratoire de Technologie Enzymatique U.R.A. n° 523 du C.N.R.S. Université de Compiègne BP 649, 60206 Compiègne Cedex, France

Philippe Guerin

U.R.A. n° 500 du C.N.R.S.-Université de Rouen Laboratorie des Substances Macromoléculaires INSA de Rouen BP 8, 76131 Mont Saint Aignan Cedex, France

Christian Braud

U.R.A. n° 500 du C.N.R.S.-Université de Rouen Laboratorie des Substances Macromoléculaires INSA de Rouen BP 8, 76131 Mont Saint Aignan Cedex, France

Michel Vert

U.R.A. n° 500 du C.N.R.S.-Université de Rouen Laboratorie des Substances Macromoléculaires INSA de Rouen BP 8, 76131 Mont Saint Aignan Cedex, France

Jean-Claude Madelmont

U71 INSERM CHR de Clermont-Ferrand BP 184, 63005 Clermont-Ferrand Cedex, France

In a first attempt to determine the fate of poly(ß-malic acid) after intravenous injection in mice, polymer end-chain ¹⁴C-radiolabelling was achieved using ¹⁴C-triethylamine as the initiator for the ring-opening polymer ization of benzyl malolactonate. The corresponding poly(ß-malic acid) sodium salt (M_w 30,000) exhibited an activity of 4.2 µCi :g^-1. Aliquots 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 exponen tially except in the liver and kidneys where a small peak was detected after 2 hours. Further investigations with poly(ß-malic acid) radiolabelled in repeat ing units will be necessary to overcome the shortcomings of the end-chain radiolabelling method applied to degradable polymers.

Journal of Bioactive and Compatible Polymers, Vol. 5, No. 4, 381-395 (1990)
DOI: 10.1177/088391159000500401


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				P. Fournie, D. Domurado, P. Guerin, C. Braud, M. Vert, and R. Pontikis In vivo Fate of Repeat-Unit-Radiolabelled Poly({beta}-malic acid), a Potential Drug Carrier Journal of Bioactive and Compatible Polymers, January 1, 1992; 7(2): 113 - 129. [Abstract] [PDF]