Abstract

Gold nanoparticles (AuNPs), which are strongly hydrophilic and dimensionally suitable for drug delivery, were used in loading and release studies of two different copper(I)-based antitumor complexes, namely [Cu(PTA)4]+ [BF4]− (A; PTA = 1, 3, 5-triaza-7-phosphadamantane) and [HB(pz)3Cu(PCN)] (B; HB(pz)3 = tris(pyrazolyl)borate, PCN = tris(cyanoethyl)phosphane). In the homoleptic, water-soluble compound A, the metal is tetrahedrally arranged in a cationic moiety. Compound B is instead a mixed-ligand (scorpionate/phosphane), neutral complex insoluble in water. In this work, the loading procedures and the loading efficiency of A and B complexes on the AuNPs were investigated, with the aim to improve their bioavailability and to obtain a controlled release. The non-covalent interactions of A and B with the AuNPs surface were studied by means of dynamic light scattering (DLS), UV–Vis, FT-IR and high-resolution x-ray photoelectron spectroscopy (HR-XPS) measurements. As a result, the AuNPs-A system proved to be more stable and efficient than the AuNPs-B system. In fact, for AuNPs-A the drug loading reached 90%, whereas for AuNPs-B it reached 65%. For AuNPs-A conjugated systems, a release study in water solution was performed over 4 days, showing a slow release up to 10%.

Highlights

  • Gold nanoparticles (AuNPs) are the most versatile material in nanotechnology, with a huge range of biological and biomedical applications, such as diagnostic, therapeutic and biosensing applications [1,2,3,4,5,6,7]

  • SCtroonncglulysihoyndsrophilic gold nanoparticles, AuNPs, were prepared to be conjugated with copper(I)

  • In the water-soluble compound A, the metal is tetrahedrally arranged in a cationic moiety, while compound B

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Summary

Introduction

Gold nanoparticles (AuNPs) are the most versatile material in nanotechnology, with a huge range of biological and biomedical applications, such as diagnostic, therapeutic and biosensing applications [1,2,3,4,5,6,7]. AuNPs have been often proposed as non-toxic carriers for drug and gene-delivery applications [8,9,10,11,12,13]. The specific properties of AuNPs, such as their high surface-to-volume ratio, peculiar optical properties, easy synthesis and versatile surface functionalization, hold pledge in the clinical field for cancer therapeutics [14,15]. AuNPs can be functionalized with different moieties, such as antibodies, peptides and/or DNA/RNA to target different cells [10,27,28], and with biocompatible molecules to prolong their in vivo circulation for drug delivery applications [29,30]. It is well known that passive targeting can be achieved by using AuNPs as a carrier, because of their preferential accumulation in tumor cells (enhanced permeability and retention (EPR) effect) [21]

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