Core crosslinked polymeric micelles from dendritic macromolecules as drug delivery agents

Abstract

Due to their biocompatibility and high loading capacity, polymeric micelles have received a lot of attention as efficient nanocarriers for drug delivery systems in recent years. Micelles from amphiphilic copolymers can be formed in aqueous media via self-assembly based on the solubility difference between hydrophilic and hydrophobic blocks. The hydrophobic segment forms the inner core and the hydrophilic segment of the block copolymer forms the shell of micelle and surrounds the core. The stability of these poly-meric micelles is very crucial to achieve the targeted drug delivery. To improve the stabil-ity of micelles resulting in increased circulation time and a more gradual release profile, many strategies have been developed to obtain crosslinked micellar architectures. In our study, we designed a biodegradable and biocompatible dendritic macromolecule based on a hydrophobic dendron segment and a hydrophilic polymer segment. We synthesized pe-riphery and focal point functionalized polyester dendron and attached to azide group con-taining PEGMA based polymers via Huisgen type ‘click’ reaction. The alkene functional-ized periphery of the polyester dendron provides crosslinkable core for the micelle. Via Thiol – Ene ‘click’ chemistry, we have been crosslinked the micellar cores and ended up with Table core crosslinked micelles. Finally, pyrene (as a mimic of hydrophobic drug) loaded core crosslinked micelles was shown to be used as a unique nanocarrier for con-trolled drug delivery systems.