POLYMERIC DRUG BY DIRECT CO-POLYMERIZATION: POLYMER OF beta -ADRENERGIC ANTAGONIST AND ITS BINDING TO RECEPTOR AND ANTIBODY.

Water-soluble polymeric drugs are often prepared by complex procedures. The same applies to the preparation of resin-anchored drugs used in the affinity chromatogrphy of drug receptors. In some instances a more direct approach may result in a considerable improvement. The authors found that inclusion of some drugs or polymeric drugs into a suitable monomer mixture and subsequent polymerization results in a useful incorporation of the compound into the newly formed polymer. The incorporation of an allyl-group containing drugs into polyacrylamide formed by a free radical polymerization was an effective process. The compounds containing quinonoid-type grouping or aromatic amines can also be incorporated into polyacrylamide; the process probably occurs by a radical substitution. Incorporation of a drug into a polymer generally changes its distribution in cells and body and their biological effects change accordingly. The direct polymerization of the drug in addition to this change leads to a further modification of properties. The main additional effects observed are based on a considerable decrease of steric accessibility of the drug after the direct incorporation into the polymeric chain. Experimental procedure is briefly described. It is concluded that the direct co-polymerization of drugs may yield products in a nearly effortless way; the resulting polymers can be easily tagged by fluorescent moieties. The process furthermore may potentially increase the specificity of a drug.

Duke Scholars

Author Robert J. Lefkowitz Medicine, Cardiology