Facteurs pharmacologiques impliqués dans l'échec thérapeutique aux inhibiteurs de la protéase du VIH-1

AIX-MARSEILLE2-BU Pharmacie (130552105) / SudocSudocFranceF

Vesicles from peptidic side-chain polymers synthesized by atom transfer radical polymerization

Block copolymers can adopt a wide range of morphologies in dilute aqueous solution. There is a significant amount of interest in the use of block copolymer vesicles for a number of applications. We show that a series of oligo(valine) and oligo(phenylalanine) peptides coupled to a methacrylic group can be prepared by conventional peptide coupling techniques. These can be successfully polymerized by atom transfer radical polymerization (ATPP) in hexafluoroisopropanol (HFIP) giving access to poly(ethylene oxide)-b-poly(side-chain peptides). Many of these polymers self-assemble to form vesicles using an organic to aqueous solvent exchange. One example with a divaline hydrophobic block gives a mixture of toroids and vesicles. Circular dichroism demonstrates that secondary structuring is observed in the hydrophobic region of the vesicle walls for the valine side-chain containing polymers

Polymersomes and their applications in cancer delivery and therapy

Polymersomes have been proposed as a platform for drug delivery systems since late 90s. They are exploited to deliver hydrophilic and/or hydrophobic therapeutic and diagnostic agents. The relatively robust membrane, the colloidal stability, along with a significant biocompatibility and easy ligands conjugation methods make polymersomes primary candidates for therapeutic drugs delivery in cancer clinical treatments. In addition, they represent an optimal choice as imaging tools in noninvasive diagnostic. As a result, polymersomes have been proposed and widely studied for anticancer treatments. However, there are not sufficient clinic translation data of human studies yet. In this critical review, we will discuss such topics, focusing on the self-assembly of membrane-forming copolymers, on their tunable physicochemical properties and on the consequential applications of these biocompatible polymersomes in drug delivery and cancer therapy