title: Synthesis of macromolecular prodrugs of procaine, histamine and isoniazid.
abstract: The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) in an aqueous medium proved to be useful in the attachment reaction. Isoniazid, procaine and histamine were covalently coupled as pendant groups onto poly-alpha,beta-aspartic acid via an amide bond. In principle, controlled release of the aforementioned drugs can be achieved by biodegradation of the polymer or by cleavage of covalently bound polymer-drug conjugates.
authors.forename: G
authors.initials: G
authors.lastname: Giammona
authors.forename: L I
authors.initials: LI
authors.lastname: Giannola
authors.forename: B
authors.initials: B
authors.lastname: Carlisi
authors.forename: M L
authors.initials: ML
authors.lastname: Bajardi
mesh_terms: D055598:Chemical Phenomena; D002621:Chemistry; D006632:Histamine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D007538:Isoniazid / Q000008:administration & dosage / Q000031:analogs & derivatives*; D008970:Molecular Weight; D011343:Procaine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D011355:Prodrugs / Q000138:chemical synthesis*
chemical_list: D011355:Prodrugs; D011343:Procaine; D006632:Histamine; D007538:Isoniazid