ISSN:
0025-116X
Keywords:
Chemistry
;
Polymer and Materials Science
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
,
Physics
Notes:
Polymer-linked 9-(2-hydroxyethoxymethyl)guanine (1) (acycloguanosine, acyclovir®) was prepared. Condensation of 1 with succinic anhydride gave in 77% yield 2-(9-guanylmethoxy)-ethyl hydrogen succinate (2), which was coupled through its carboxylic group either to poly(L-lysine) (M̄r = 55000) or to N-(6-aminohexyl)carbamoylmethylated dextran T80 to yield the polymers 3 and 4 (ligand concentrations in 3: 30 - 48 μmol of 2/g, in 4: 100 - 171 μmol of 2/g). From both polymers the antiviral 1 could be released by controlled saponification; the rate of drug delivery was found to be a function of pH and temperature. The polymeric carrier system 3 was degraded by endo-dextranase, and the carrier system 4 by trypsin, yielding low-molecular-weight derivatives of the pharmacon.
Additional Material:
3 Ill.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/macp.1984.021850407
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