Abstract

We report on the synthesis and evaluation of biopolymeric spheres of poly(lactide-co-glycolide) containing different amounts of magnetite nanoparticles and Ibuprofen (PLGA-Fe3O4-IBUP), but also chitosan (PLGA-CS-Fe3O4-IBUP), to be considered as drug delivery systems. Besides morphological, structural, and compositional characterizations, the PLGA-Fe3O4-IBUP composite microspheres were subjected to drug release studies, performed both under biomimetically-simulated dynamic conditions and under external radiofrequency magnetic fields. The experimental data resulted by performing the drug release studies evidenced that PLGA-Fe3O4-IBUP microspheres with the lowest contents of Fe3O4 nanoparticles are optimal candidates for triggered drug release under external stimulation related to hyperthermia effect. The as-selected microspheres and their chitosan-containing counterparts were biologically assessed on macrophage cultures, being evaluated as biocompatible and bioactive materials that are able to promote cellular adhesion and proliferation. The composite biopolymeric spheres resulted in inhibited microbial growth and biofilm formation, as assessed against Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans microbial strains. Significantly improved antimicrobial effects were reported in the case of chitosan-containing biomaterials, regardless of the microorganisms’ type. The nanostructured composite biopolymeric spheres evidenced proper characteristics as prolonged and controlled drug release platforms for multipurpose biomedical applications.

Highlights

  • The personalized therapy desideratum aims for an accurate and controllable local distribution of therapeutic agents, and to ensure the specific and selective targeting of the molecular or cellular receptors [1,2]

  • In order to evaluate the antimicrobial effects exhibited by nanostructured biopolymeric spheres, we only considered the most promising poly(lactic-co-glycolic) acid (PLGA)-Fe3 O4 -IBUP systems and their CS-containing corresponding counterparts, namely PLGA-CS-Fe3 O4 -IBUP

  • PLGA-Fe3 O4 -IBUP Biopolymeric Spheres. As it can be noticed in the Transmission Electron Microscopy (TEM) micrograph (Figure 2a), the modified co-precipitation synthesis method enabled the formation of nanosized magnetite particles, with preferential spheroidal shape

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Summary

Introduction

The personalized therapy desideratum aims for an accurate and controllable local distribution of therapeutic agents, and to ensure the specific and selective targeting of the molecular or cellular receptors [1,2]. Nanoparticle-based drug formulations have proved their potential to deal with challenging diseases. Materials 2019, 12, 2521 studies performed on nanoparticles designed for drug delivery applications in 2018 (5563 in Pubmed [9], 29,789 in Scopus [10], and 9165 in ScienceDirect [11]; entries searched in July 2019). Nanoparticles have revolutionized how drugs are formulated, delivered, and explored for specific and selective therapies, and they are currently utilized in diagnosis, cancer therapy, HIV and AIDS therapy, nutraceutical delivery, anti-bacterial systems, etc. Polymer particles or capsules are proper choices for modern pharmacotherapy, thanks to their intrinsic physicochemical versatility and tunable functionality, which enable higher loading and encapsulation efficiency of various therapeutics (such as phytochemical and drug molecules, proteins, growth factors, genes, and cells) and controllable or/and triggerable release mechanisms [15,16]

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