Impact of Branching on the Solution Behavior and Serum Stability of Starlike Block Copolymers

April 9, 2019

Title

Impact of Branching on the Solution Behavior and Serum Stability of Starlike Block Copolymers

Author

Regina Holm, Marcel Douverne, Benjamin Weber, Tobias Bauer, Andreas Best, Patrick Ahlers, Kaloian Koynov, Pol Besenius, Matthias Barz

Year

2018

Journal

Biomacromolecules

Abstract

The size control of nanomedicines for tumor diagnosis and therapy is of high importance, since it enables or disables deep and sufficient tumor penetration. Amphiphilic star-shaped block copolypept(o)ides offer substantial promise to precisely adjust the hydrophobic core and the hydrophilic corona, independent of each other, and therefore simultaneously control the size dimension in the interesting size range from 10 to 30 nm. To gain access to core–shell structures of such sizes, 3-arm and 6-arm PeptoStars, based on poly(γ-tert-butyloxycarbonyl-l-glutamate)-b-polysarcosine (pGlu(OtBu)-b-pSar), were prepared via controlled living ring-opening polymerization (ROP) of the corresponding N-carboxyanhydrides. Moreover, size exclusion chromatography (SEC) proves the presence of well-defined star shaped polymers with molecular weights from 38 to 88 kg/mol with low polymer dispersities of 1.16 to 1.23. By varying the α-helical peptide core and maintain a constant polysarcosine corona, hydrodynamic size analyses revealed the importance of using a sufficiently large and dense hydrophilic shielding corona to prevent aggregation of the hydrophobic core and obtain uniform-sized spherical-shaped particles with hydrodynamic diameters below 24 nm. Fluorescence correlation spectroscopy (FCS) additionally demonstrates the absence of protein adsorption in human plasma for 6-arm polypept(o)ide stars and thus confirms polysarcosine as stealthlike material.

Instrument

J-815

Keywords

Circular dichroism, Secondary structure, Chemical stability, Polymers, Biochemistry