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pubmed-article:18288803pubmed:abstractTextA combination of controlled radical polymerization and azide-alkyne click chemistry was employed to prepare temperature-responsive block copolymer micelles conjugated with biological ligands with potential for active targeting of cancer tissues. Block copolymers of N-isopropylacrylamide (NIPAM) and N,N-dimethylacrylamide (DMA) were synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization with an azido chain transfer agent (CTA). Pseudo-first-order kinetics and linear molecular weight dependence on conversion were observed for the RAFT polymerizations. CuI-catalyzed coupling with propargyl folate resulted in folic acid residues being efficiently conjugated to the alpha-azido chain ends of the homo and block copolymers. Temperature-induced self-assembly resulted in aggregates capable of controlled release of a model hydrophobic drug. CuI-catalyzed azide-alkyne cycloaddition has proven superior to conventional methods for conjugation of biological ligands to macromolecules, and the general strategy presented herein can potentially be extended to the preparation of folate-functionalized assemblies with other stimuli susceptibility (e.g., pH) for therapeutic and imaging applications.lld:pubmed
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pubmed-article:18288803pubmed:dateRevised2008-11-21lld:pubmed
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pubmed-article:18288803pubmed:year2008lld:pubmed
pubmed-article:18288803pubmed:articleTitleFolate-conjugated thermoresponsive block copolymers: highly efficient conjugation and solution self-assembly.lld:pubmed
pubmed-article:18288803pubmed:affiliationDepartment of Chemistry, Southern Methodist University, 3215 Daniel Avenue, Dallas, Texas 75275-0314, USA.lld:pubmed
pubmed-article:18288803pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:18288803pubmed:publicationTypeResearch Support, U.S. Gov't, Non-P.H.S.lld:pubmed
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