title: Drug Release by Direct Jump from Poly(ethylene-glycol-b-ε-caprolactone) Nano-Vector to Cell Membrane.
abstract: Drug delivery by nanovectors involves numerous processes, one of the most important being its release from the carrier. This point still remains unclear. The current work focuses on this point using poly(ethyleneglycol-b-ε-caprolactone) micelles containing either pheophorbide-a (Pheo-a) as a fluorescent probe and a phototoxic agent or fluorescent copolymers. This study showed that the cellular uptake and the phototoxicity of loaded Pheo-a are ten times higher than those of the free drug and revealed a very low cellular penetration of the fluorescence-labeled micelles. Neither loaded nor free Pheo-a displayed the same cellular localization as the labeled micelles. These results imply that the drug entered the cells without its carrier and probably without a disruption, as suggested by their stability in cell culture medium. These data allowed us to propose that Pheo-a directly migrates from the micelle to the cell without disruption of the vector. This mechanism will be discussed.
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. till@chimie.ups-tlse.fr.
authors.forename: Ugo
authors.initials: U
authors.lastname: Till
authors.affiliation: Université de Toulouse, Equipe de Biophysique Cellulaire, IPBS-CNRS UMR5089 205, Route de Narbonne BP 64182, 31077 Toulouse, France. laure.gibot@ipbs.fr.
authors.forename: Laure
authors.initials: L
authors.lastname: Gibot
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. afmingo@chimie.ups-tlse.fr.
authors.forename: Anne-Françoise
authors.initials: AF
authors.lastname: Mingotaud
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. jehrhart@hotmail.fr.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Ehrhart
authors.affiliation: Université de Toulouse, Equipe de Biophysique Cellulaire, IPBS-CNRS UMR5089 205, Route de Narbonne BP 64182, 31077 Toulouse, France. lucwasungu@yahoo.com.
authors.forename: Luc
authors.initials: L
authors.lastname: Wasungu
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. cmingo@chimie.ups-tlse.fr.
authors.forename: Christophe
authors.initials: C
authors.lastname: Mingotaud
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. souchard@chimie.ups-tlse.fr.
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Souchard
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. poinso@chimie.ups-tlse.fr.
authors.forename: Alix
authors.initials: A
authors.lastname: Poinso
authors.affiliation: Université de Toulouse, Equipe de Biophysique Cellulaire, IPBS-CNRS UMR5089 205, Route de Narbonne BP 64182, 31077 Toulouse, France. rols@ipbs.fr.
authors.forename: Marie-Pierre
authors.initials: MP
authors.lastname: Rols
authors.affiliation: Université de Toulouse, Laboratoire de Chimie Agro-industrielle (LCA), INRA, INPT, INP-EI PURPAN, 31076 Toulouse, France. frederic.violleau@purpan.fr.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Violleau
authors.affiliation: Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France. vicendo@chimie.ups-tlse.fr.
authors.forename: Patricia
authors.initials: P
authors.lastname: Vicendo
mesh_terms: D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D002734:Chlorophyll / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D065546:Drug Liberation; D045325:HCT116 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D007783:Lactones / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D008823:Micelles; D017319:Photosensitizing Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D007783:Lactones; D008823:Micelles; D017319:Photosensitizing Agents; C521904:poly(ethylene glycol)-block-poly(epsilon-caprolactone); D002734:Chlorophyll; D011092:Polyethylene Glycols; C032623:pheophorbide a
keywords: cellular penetration; pheophorbide-a; polymer micelles; uptake mechanism