Abstract

The aim of our study was to develop a novel method for the preparation of polymeric core-shell nanoparticles loaded with various actives for biomedical applications. Poly(caprolactone) (PCL), poly(lactic acid) (PLA) and poly(lactide-co-glycolide) (PLGA) nanoparticles were prepared using the spontaneous emulsification solvent evaporation (SESE) method. The model active substance, Coumarin-6, was encapsulated into formed polymeric nanoparticles, then they were modified/functionalized by multilayer shells’ formation. Three types of multilayered shells were formed: two types of polyelectrolyte shell composed of biocompatible and biodegradable polyelectrolytes poly-L-lysine hydrobromide (PLL), fluorescently-labeled poly-L-lysine (PLL-ROD), poly-L-glutamic acid sodium salt (PGA) and pegylated-PGA (PGA-g-PEG), and hybrid shell composed of PLL, PGA, and SPIONs (superparamagnetic iron oxide nanoparticles) were used. Multilayer shells were constructed by the saturation technique of the layer-by-layer (LbL) method. Properties of our polymeric core-shell nanoparticle were optimized for bioimaging, passive and magnetic targeting.

Highlights

  • Numerous new chemicals have been developed to treat various complicated diseases effectively, but at the same time, some of them produce serious side effects, proving that the benefit does not always outweigh the risk [1,2]

  • The early nanoparticles were mainly formulated from poly(alkylcyanoacrylate), currently the most widely used polymers for nanoparticles have been: from natural proteins or polysaccharides e.g., chitosan, alginate; and synthetic polymers e.g., poly(lactic acid) (PLA), poly(glycolic acid) (PGA), and their copolymers, poly(lactide-co-glycolide) (PLGA) [1,5,6,7,8]

  • In the emulsification/solvent evaporation technique selected polymer is dissolved in an organic solvent and this mixture is dispersed into an aqueous solution to make oil in water nanoemulsion by using a surfactant agent

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Summary

Introduction

Numerous new chemicals have been developed to treat various complicated diseases effectively, but at the same time, some of them produce serious side effects, proving that the benefit does not always outweigh the risk [1,2]. The initial therapeutic effect of drug-loaded nanoparticles was relatively poor due to rapid clearance of the particles by phagocytosis post-intravenous administration. In recent years, this problem has been solved by the proper surface modification of nanoparticles e.g., by grafting their surface with many hydrophilic and flexible polymers. It was found that under certain pathological states, such as tumors, infarcts, and inflammation, the permeability of vascular endothelial increases and they become leaky In such regions with increased vascular permeability, nanoparticles can accumulate and exert their therapeutic effect. In magnetic-sensitive systems, iron oxide nanoparticles referred to as superparamagnetic iron oxide nanoparticles (SPIONs) with particle size 4–10 nm are used

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