Polymer-biologically active principle conjugates obtained by esterification of poly(vinyl alcohol)

The paper deals with the study of some polymer-biologically active principle systems characterized by the controlled release of the bioactive component by hydrolyze followed by diffusion. The systems were obtained by coupling the 2-mercapto-benzotiazolylacetic acid and N-(m-nitrobenzoyl)-L-methionine on poly(vinyl alcohol) by means of esteric bonds in the presence of diciclohexylcarbodiimide as an activator. The influence of some coupling process parameters on the reaction efficiency was studied, such as the drug/support and activator/support ratios. The coupling products with a maximum content of biologically active compound were characterized by spectral measurements, also as regards the capacity of bioactive compound release under the conditions simulating those within the gastro-intestinal tract. The antibacterial activity of the conjugates against Staphylococcus aureus, Eschrichia coli, Sarcina lutea, and Bacillus subtilis was determined.