Novel small molecule compounds in pharmaceutical research can be identified by high-throughput screening or structure based design. Frequently those lead structures suffer from restrictions in applicability and ease of approval due to unfavorable properties e.g. water insolubility. Therefore, much effort is spend, including cost-intensive structure optimization cycles, to overcome these drawbacks.Polymer-block-peptides are especially suited to render insoluble drugs water-soluble, without the need to structurally adapt the small molecule entity.[1]A generic approach is presented for advanced tailoring of polymer drug carriers based on polymer-block-peptides to develop specific drug formulation agents.[2] Combinatorial means are used to select suitable peptide segments to specifically complex small molecule drugs. Precise adjustment of drug-release profiles can be programmed in the peptide segment, which can be considered as an improvement over established block-copolymer carriers.Proof of principle is shown on the photosensitizer m-tetra(hydroxyphenyl)chlorine (m-THPC) as a partially approved drug for photodynamic cancer therapy. To assist the design of peptide-block-poly(ethylene oxide) copolymers, a fluorescence-based screening method was established. Solubilization capacity and release kinetics from the transport system proved to depend strongly on the peptide sequence of the peptide-PEO conjugates.[1] Anna K. H. Hirsch, Fran�ois Diederich, Markus Antonietti, Hans G. B�rner, Soft Matter 2010  , 6, 88�91.[2] Sebastian Wieczorek, Eberhard Krause, Steffen Hackbarth, Beate R�der, Anna K. H. Hirsch, Hans G. B�rner, J. Am. Chem. Soc. 2013  , 135, 1711-1714.

Screening for specific interactions: Precisely tailored drug transporters for small molecule solubilization and release

246th National Meeting (2013)

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