6533b7d2fe1ef96bd125f725

RESEARCH PRODUCT

Pentafluorophenyl Ester-based Polymersomes as Nanosized Drug-Delivery Vehicles

Thomas FritzKarl FischerKristin MohrRudolf ZentelMartin SchererRaphael ThiermannFrank Depoix

subject

PolymersomesMaterials sciencePolymers and Plastics02 engineering and technology010402 general chemistryMethacrylate01 natural scienceschemistry.chemical_compoundAminolysisHPMAPolymer chemistryMaterials ChemistryMethacrylamideReversible addition−fragmentation chain-transfer polymerizationRAFT polymerizationVesicleOrganic Chemistry021001 nanoscience & nanotechnologyCombinatorial chemistry0104 chemical scienceschemistrydrug deliveryPolymersomeDrug deliveryactivated esters0210 nano-technologyDrug carrier

description

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.

https://doi.org/10.1002/marc.201500444