title: Smart nanocarriers for pH-triggered targeting and release of hydrophobic drugs.
abstract: The use of hybrid pH-sensitive micelles based mainly on the (PEO)(129)(P2VP)(43)(PCL)(17) ABC miktoarm star copolymer as potential triggered drug delivery systems was investigated. Co-micellization of this star copolymer with a second copolymer labeled by a targeting ligand, i.e. biotin, on the pH sensitive block (poly-2-vinylpyridine) is considered here in order to impart possible active targeting of the tumor cells. Two architectures were studied for these labeled copolymers, i.e. a miktoarm star or a linear ABC terpolymer, and the respective hybrid micelles are compared in terms of cytotoxicity (cells viability) and cellular uptake (using fluorescent dye loaded micelles). Finally, the triggered drug release in the cytosol of tumor cells was investigated by studying, on the one hand, the lysosomal integrity after internalization and, on the other hand, the release profile in function of the pH.
authors.affiliation: Center for Education and Research on Macromolecules, University of Liege, B6 Sart-Tilman, B-4000 Liege, Belgium. c.jerome@ulg.ac.be
authors.forename: S
authors.initials: S
authors.lastname: Cajot
authors.forename: K
authors.initials: K
authors.lastname: Van Butsele
authors.forename: A
authors.initials: A
authors.lastname: Paillard
authors.forename: C
authors.initials: C
authors.lastname: Passirani
authors.forename: E
authors.initials: E
authors.lastname: Garcion
authors.forename: J P
authors.initials: JP
authors.lastname: Benoit
authors.forename: S K
authors.initials: SK
authors.lastname: Varshney
authors.forename: C
authors.initials: C
authors.lastname: Jérôme
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008247:Lysosomes / Q000378:metabolism; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry / Q000494:pharmacology; D051381:Rats
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011145:Polyvinyls