Soluble Camptothecin Derivatives Prepared by Click Cycloaddition Chemistry on Functional Aliphatic Polyesters

Autor: Todd Emrick, Bryan Parrish
Rok vydání: 2006
Předmět:
Zdroj: Bioconjugate Chemistry. 18:263-267
ISSN: 1520-4812
1043-1802
DOI: 10.1021/bc060201d
Popis: Aliphatic polyesters are of interest as biomaterials and drug-delivery vehicles, as their ability to degrade under physiological conditions provides a mechanism for both drug release and clearance of the polymer from the body. Presented here is the synthesis of a polyester-drug graft copolymer conjugate, enabled by click cycloaddition of azide-functionalized camptothecin derivatives with alkyne-functionalized aliphatic polyesters. Further grafting of residual alkyne groups with azide-terminated poly(ethylene oxide) gave a water-soluble polyester-camptothecin conjugate. Control over PEGylation and drug loading, inherent to the graft copolymer design, opens versatile routes to new materials with potential utility in polymer therapeutics.
Databáze: OpenAIRE