Abstract
In this work, a method to prepare hybrid amphiphilic block copolymers consisting of biocompatible synthetic glycopolymer with non-degradable backbone and biodegradable poly(amino acid) (PAA) was developed. The glycopolymer, poly(2-deoxy-2-methacrylamido-D-glucose) (PMAG), was synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization. Two methods for modifying the terminal dithiobenzoate-group of PMAG was investigated to obtain the macroinitiator bearing a primary aliphatic amino group, which is required for ring-opening polymerization of N-carboxyanhydrides of hydrophobic α-amino acids. The synthesized amphiphilic block copolymers were carefully analyzed using a set of different physico-chemical methods to establish their composition and molecular weight. The developed amphiphilic copolymers tended to self-assemble in nanoparticles of different morphology that depended on the nature of the hydrophobic amino acid present in the copolymer. The hydrodynamic diameter, morphology, and cytotoxicity of polymer particles based on PMAG-b-PAA were evaluated using dynamic light scattering (DLS) and transmission electron microscopy (TEM), as well as CellTiter-Blue (CTB) assay, respectively. The redox-responsive properties of nanoparticles were evaluated in the presence of glutathione taken at different concentrations. Moreover, the encapsulation of paclitaxel into PMAG-b-PAA particles and their cytotoxicity on human lung carcinoma cells (A549) and human breast adenocarcinoma cells (MCF-7) were studied.
Highlights
The development of polymer nanoparticles as drug delivery and detection systems has been extensively investigated [1,2,3]
The conjugation of water-soluble PMAG and hydrophobic poly(amino acids) represents a great challenge due to the impossibility to combine both polymers in the homogeneous reaction medium appropriate for conjugation
It is related to the poor solubility of ordered hydrophobic poly(amino acids) even in organic media
Summary
The development of polymer nanoparticles as drug delivery and detection systems has been extensively investigated [1,2,3]. The main advantages of polymer systems compared to inorganic materials are the variety of their structure and properties, the higher drug loading capacities, and the diversity of reactive functional groups for the attachment of biomolecule-vectors. Among the wide range of biocompatible and biodegradable polymers utilized for preparation of nanoparticles, amphiphilic copolymers allow for the simple formation of nanostructures of different morphology (polymersomes, micelles, nanospheres) due to their ability to self-assemble in aqueous media [4,5,6]. A wide variety of amphiphilic copolymers of different structure and composition have been described and discussed [4,10,11].
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