High-throughput (HT) experimentation represents a fast and efficient tool for the preparation and characterization of materials for diverse pharmaceutical applications such as basic structure-property relationships of polymers and their drug and gene delivery potential. Influencing factors for the formation of polymeric nanoparticles by nanoprecipitation can be analyzed in a fast and efficient manner by using liquid handling robots and HT-DLS. We show that the polymer molar mass as well as polymer-solvent interactions have a significant influence on the nanoprecipitation behavior. A further application field is a HT workflow for gene delivery in vitro. In detail, complex preparation (polymer and genetic material), complex size, DNA binding affinity, complex stability, cytotoxicity, and transfection efficiency can be investigated via HT- assays. To proof the usage of the investigated workflow, various poly(ethylene imine)s (PEI) of linear and branched architecture and different molar masses as well as plasmid DNA as genetic material were used as representative polymer and genetic material, respectively.This approach allows the testing of many different polymers and parameters concerning biological outcomes as transfection properties or cytotoxicity, and yields faster insights into structure-property relationships for biological activity.   Figure 1. Schematic representation of the HT preparation and screening of polyplex formulations. References:1. I. Perevyazko, A. Vollrath, C. Pietsch, S. Schubert, G. M. Pavlov, U. S. Schubert J. Polym. Sci. Part A, Polym. Chem. 2012 , 50, 2906-2913.2. A. C. Rinkenauer, A. Vollrath, A. Schallon, L. Tauhardt, K. Kempe, S. Schubert, D. Fischer, U. S. Schubert ACS Comb. Sci. 2013 , 15, 475-482.

High-throughput formulation of nanoparticles and polyplexes for structure-property investigations

248th National Meeting (2014)

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