Collect. Czech. Chem. Commun. 1988, 53, 1078-1085

In vitro release of chloramphenicol from poly[N-(2-hydroxypropyl)methacrylamide] carriers by Cathepsin B

Karel Ulbricha, Olga Nazarovaa, Eugenii Panarina, Miroslav Baudyšb and Michail V. Solovskiic

a Institute of Macromolecular Chemistry, Czechoslovak Academy of Sciences, 162 06 Prague 6, Czechoslovakia
b Institute of Organic Chemistry and Biochemistry, Czechoslovak Academy of Sciences, 166 10 Prague 6, Czechoslovakia
c Institute of Macromolecular Compounds, Academy of Sciences of the U.S.S.R., 199 004 Leningrad, U.S.S.R.


It has been shown in recent years that copolymers of N-(2-hydroxypropyl)methacrylamide may be used as targeted polymer drug carriers. The wide-spectrum antibiotic chloramphenicol has been bound to these carriers by means of biodegradable oligopeptidic sequences. The rate of drug release from the carrier in aqueous buffer solutions pH 7·4 and 6·0 was measured and the rates were compared with that of the enzymatic drug release from the carrier by means of the enzyme Cathepsin B. It was shown that the active drug may be released from the carrier by simple hydrolysis or by acting with an enzyme and that the rate of drug release depends on the structure of the oligopeptidic sequence which acts as a link between the drug and the polymer. The results obtained may be employed in the synthesis of a polymer compound potentially possessing antimicrobial activity.