title: Click chemistry for drug delivery nanosystems.
abstract: The purpose of this Expert Review is to discuss the impact of click chemistry in nanosized drug delivery systems. Since the introduction of the click concept by Sharpless and coworkers in 2001, numerous examples of click reactions have been reported for the preparation and functionalization of polymeric micelles and nanoparticles, liposomes and polymersomes, capsules, microspheres, metal and silica nanoparticles, carbon nanotubes and fullerenes, or bionanoparticles. Among these click processes, Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) has attracted most attention based on its high orthogonality, reliability, and experimental simplicity for non-specialists. A renewed interest in the use of efficient classical transformations has been also observed (e.g., thiol-ene coupling, Michael addition, Diels-Alder). Special emphasis is also devoted to critically discuss the click concept, as well as practical aspects of application of CuAAC to ensure efficient and harmless bioconjugation.
authors.affiliation: Department of Organic Chemistry, Center for Research in Biological Chemistry & Molecular Materials (CIQUS), University of Santiago de Compostela, Jenaro de la Fuente s/n, 15782 Santiago de Compostela, Spain.
authors.forename: Enrique
authors.initials: E
authors.lastname: Lallana
authors.forename: Ana
authors.initials: A
authors.lastname: Sousa-Herves
authors.forename: Francisco
authors.initials: F
authors.lastname: Fernandez-Trillo
authors.forename: Ricardo
authors.initials: R
authors.lastname: Riguera
authors.forename: Eduardo
authors.initials: E
authors.lastname: Fernandez-Megia
mesh_terms: D000480:Alkynes / Q000737:chemistry*; D000906:Antibodies / Q000737:chemistry; D001386:Azides / Q000737:chemistry*; D002384:Catalysis; D057930:Click Chemistry; D003300:Copper / Q000737:chemistry*; D003500:Cyclization; D016503:Drug Delivery Systems; D006801:Humans; D008055:Lipids / Q000737:chemistry; D050997:Nanomedicine; D053758:Nanoparticles / Q000737:chemistry*; D009696:Nucleic Acids / Q000737:chemistry; D010455:Peptides / Q000737:chemistry; D011134:Polysaccharides / Q000737:chemistry; D011506:Proteins / Q000737:chemistry
chemical_list: D000480:Alkynes; D000906:Antibodies; D001386:Azides; D008055:Lipids; D009696:Nucleic Acids; D010455:Peptides; D011134:Polysaccharides; D011506:Proteins; D003300:Copper