Soluble Camptothecin Derivatives Prepared by Click Cycloaddition Chemistry on Functional Aliphatic Polyesters
Bioconjugate Chemistry2006Vol. 18(1), pp. 263–267
Citations Over TimeTop 10% of 2006 papers
Abstract
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.
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