Self-assembled core-shell micelles from peptide-b-polymer molecular chimeras towards structure-activity relationships

Charlotte Drappier (1, 2) , Hugo de Oliveira (2) , Olivier Sandre (2, 3) , Emmanuel Ibarboure (2) , Sophie Combet (4) , Elisabeth Garanger (2, 3) , Sébastien Lecommandoux (2, 3)

1 IECB - Institut Européen de Chimie et de Biologie
2 LCPO - Laboratoire de Chimie des Polymères Organiques
3 Team 3 LCPO : Polymer Self-Assembly & Life Sciences
4 LLB - UMR 12 - Laboratoire Léon Brillouin

The aim of this contribution is to design, produce and characterize size-tuneable core-shell micelles from amphiphilic Tat-b-poly(trimethylene carbonate) (Tat-b-PTMC) molecular chimeras, and to explore their biological properties. Because the extensive characterization of nanomaterials is a pre-requisite to understand and rationalize their ensuing properties, we present a detailed description of Tat-b-PTMC micelles thanks to light scattering, AFM imaging and small angle neutron scattering analyses. In vitro, Tat-b-PTMC micelles were found to be rapidly and efficiently internalized by HeLa cells, with cellular uptake kinetics being mostly related to Tat peptide content and, to a lesser extent, to nanoparticle size. We also demonstrated that, after a first membrane-binding step, Tat-b-PTMC micelles were taken up by cells via an energy-dependent endocytotic process.

Mots clés: NANOPARTICLES; DESIGN; DELIVERY; MECHANISM; BLOCK-COPOLYMERS; CELLULAR UPTAKE; TAT PEPTIDE; HIV-1 TAT; SCATTERING; CYTOTOXICITY

Domaines: Polymères

Charlotte Drappier, Hugo de Oliveira, Olivier Sandre, Emmanuel Ibarboure, Sophie Combet, et al.. Self-assembled core-shell micelles from peptide-b-polymer molecular chimeras towards structure-activity relationships. Faraday Discussions, 2013, 166, pp.83-100. ⟨10.1039/c3fd00098b⟩. ⟨hal-00959583⟩