Novel poly(chloromethylstyrene)/polyglycidol conjugates obtained by metal-free click reactions for the development of drug delivery systems

Novel poly(chloromethylstyrene)/polyglycidol conjugates obtained by metal-free click reactions for the development of drug delivery systems

Poster

Krasimira Rusinova-Ilieva 1,2, Erik Dimitrov 1, Natalia Toncheva-Moncheva 1*, Stanislav Rangelov 1*
1Institute of Polymers, Bulgarian Academy of Sciences, Sofia, Bulgaria
2Faculty of Physics, Sofia University “St. Kliment Ohridski”, Sofia, Bulgaria

One-third of drugs and biological active substances (BAS) in development are water insoluble and one-half fail in trials because of poor pharmacokinetics. This limits its applications, since it hinders both the formulation of stable drug dosage forms and its bioavailability. Copolymer micelles are nanosized particles that can solubilize hydrophobic drugs or BAS and alter their kinetics in vitro and in vivo. The present study is focused on the development and characterization of polymeric nanocarriers as a delivery platform for hydrophobic drugs and BAS. Poly(chloromethylstyrene)/polyglycidol based copolymers, in particular (PCMS/PG), the PCMS-b-PS/PG and P(CMS-co-S)/PG were applied for the preparation of the micelle-based nanocarriers. The copolymers were prepared by initiator free “click” coupling reactions of appropriately functionalized polyglycidol with synthetic polymer chains of different chemical nature, composition, and properties, namely, poly(chloromethylstyrene)s. Nitroxide mediated controlled radical polymerization was used to synthesize the poly(chloromethyl styrene) (PCMS) homopolymer, the PCMS-b-PS block copolymer and the P(CMS-co-S) random copolymer. Further, they were functionalized with azido functional groups and conjugated with polyglycidol. Resulting copolymers are amphiphilic and form well-defined stable nano sized micelles in aqueous solution. The nanoparticles were thoroughly investigated by a variety of techniques –FTIR, 1H NMR, UV light measurement, static, dynamic, and electrophoretic light scattering.
Keywords: drug delivery, micelles, nanoparticles, click reaction, CMC