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Molecules 2016, 21(12), 1643;

Drug Release by Direct Jump from Poly(ethylene-glycol-b-ε-caprolactone) Nano-Vector to Cell Membrane

Université de Toulouse, UPS/CNRS, IMRCP, 118 Rte de Narbonne, 31062 Toulouse, France
Université de Toulouse, Equipe de Biophysique Cellulaire, IPBS-CNRS UMR5089 205, Route de Narbonne BP 64182, 31077 Toulouse, France
Université de Toulouse, Laboratoire de Chimie Agro-industrielle (LCA), INRA, INPT, INP-EI PURPAN, 31076 Toulouse, France
Author to whom correspondence should be addressed.
Academic Editor: Tommasina Coviello
Received: 24 October 2016 / Revised: 15 November 2016 / Accepted: 18 November 2016 / Published: 30 November 2016
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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. View Full-Text
Keywords: polymer micelles; pheophorbide-a; cellular penetration; uptake mechanism polymer micelles; pheophorbide-a; cellular penetration; uptake mechanism

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Till, U.; Gibot, L.; Mingotaud, A.-F.; Ehrhart, J.; Wasungu, L.; Mingotaud, C.; Souchard, J.-P.; Poinso, A.; Rols, M.-P.; Violleau, F.; Vicendo, P. Drug Release by Direct Jump from Poly(ethylene-glycol-b-ε-caprolactone) Nano-Vector to Cell Membrane. Molecules 2016, 21, 1643.

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