title: Pentafluorophenyl Ester-based Polymersomes as Nanosized Drug-Delivery Vehicles.
abstract: In this work, activated ester chemistry is employed to synthesize biocompatible and readily functionalizable polymersomes. Via aminolysis of pentafluorophenyl methacrylate-based precursor polymers, an N-(2-hydroxypropyl) methacrylamide (HPMA)-analog hydrophilic block is obtained. The precursor polymers can be versatile functionalized by simple addition of suitable primary amines during aminolysis as demonstrated using a fluorescent dye. Vesicle formation is proven by cryoTEM and light scattering. High encapsulation efficiencies for hydrophilic cargo like siRNA are achieved using dual centrifugation and safe encapsulation is demonstrated by gel electrophoresis. In vitro studies reveal low cytotoxicity and no protein adsorption-induced aggregation in human blood serum occurs, making the vesicles interesting candidates as nanosized drug carriers.
authors.affiliation: Institute of Organic Chemistry, Johannes Gutenberg University Mainz, Duesbergweg 10-14, 55099, Mainz, Germany.
authors.forename: Martin
authors.initials: M
authors.lastname: Scherer
authors.affiliation: Institute of Physical Chemistry, Johannes Gutenberg University Mainz, Jakob-Welder-Weg 11, 55099, Mainz, Germany.
authors.forename: Karl
authors.initials: K
authors.lastname: Fischer
authors.affiliation: Institute of Zoology, Johannes Gutenberg University Mainz, J.-J.-Becher-Weg 7, 55128, Mainz, Germany.
authors.forename: Frank
authors.initials: F
authors.lastname: Depoix
authors.affiliation: Institute of Pharmacy and Biochemistry, Johannes Gutenberg University Mainz, Staudinger Weg 5, 55128, Mainz, Germany.
authors.forename: Thomas
authors.initials: T
authors.lastname: Fritz
authors.affiliation: Fraunhofer ICT-IMM, Carl-Zeiss-Str. 18-20, 55129, Mainz, Germany.
authors.forename: Raphael
authors.initials: R
authors.lastname: Thiermann
authors.affiliation: Max Planck Institute for Polymer Research, Ackermannweg 10, 55128, Mainz, Germany.
authors.forename: Kristin
authors.initials: K
authors.lastname: Mohr
authors.affiliation: Institute of Organic Chemistry, Johannes Gutenberg University Mainz, Duesbergweg 10-14, 55099, Mainz, Germany.
authors.forename: Rudolf
authors.initials: R
authors.lastname: Zentel
keywords: HPMA; RAFT polymerization; activated esters; drug delivery; polymersomes