LAUSR

Amphiphilic block copolymers with a thermoresponsive poly(N-isopropylacrylamide) block and a glycopeptide block were synthesized and particle formation as well as interaction of the glyco-corona with lectins was investigated. The synthetic route comprises the preparation of block copolymer by N-carboxyanhydride polymerization and subsequent deprotection to obtain pH- and thermoresponsive poly(l-glutamic acid)-b-poly(N-isopropylacrylamide) (pGA-b-pNIPAM), which was then further modified with different amino sugars by a versatile coupling method with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholin-4-ium chloride (DMT-MM). The glycosylated pGA-b-pNIPAM block copolymers were investigated with regard to cloud point temperatures (Tcp ), particle size and stability. The morphology of the particles was visualized using cryo-SEM. Zeta potential measurements were indicating that the saccharide moieties are located on the surface of the particles. This assumption was further substantiated by quantitative lectin interaction assays with non-aggregated and aggregated glycosylated pGA-b-pNIPAM. The interaction of the model lectin ConA with the block copolymers was independent of the degree of substitution in the non-aggregated state at room temperature. However, at 37°C, when particles of pGA-b-pNIPAM were present, the interaction became stronger with increasing degree of substitution. This interaction with lectins can be used for targeting saccharide-modified particles in drug delivery. This article is protected by copyright. All rights reserved.