Abstract
Strongly hydrophilic gold nanoparticles (AuNPs), functionalized with citrate and L-cysteine, were synthetized and used as Resveratrol (RSV) vehicle to improve its bioavailability. Two different conjugation procedures were investigated: the first by adding RSV during AuNPs synthesis (1) and the second by adding RSV after AuNPs synthesis (2). The two different conjugated systems, namely AuNPs@RSV1 and AuNPs@RSV2 respectively, showed good loading efficiency (η%): η1 = 80 ± 5% for AuNPs@RSV1 and η2 = 20 ± 3% for AuNPs@RSV2. Both conjugated systems were investigated by means of Dynamic Light Scattering (DLS), confirming hydrophilic behavior and nanodimension (<2RH> 1 = 45 ± 12 nm and <2RH> 2 = 170 ± 30 nm). Fourier Transform Infrared Spectroscopy (FT-IR), Synchrotron Radiation induced X-Ray Photoelectron Spectroscopy (SR-XPS) and Near Edge X-ray Absorption Fine Structure (NEXAFS) techniques were applied to deeply understand the hooking mode of RSV on AuNPs surface in the two differently conjugated systems. Moreover, the biocompatibility of AuNPs and AuNPs@RSV1 was evaluated in the concentration range 1.0–45.5 µg/mL by assessing their effect on breast cancer cell vitality. The obtained data confirmed that, at the concentration used, AuNPs do not induce cell death, whereas AuNPs@RSV1 maintains the same anticancer effects as the unconjugated RSV.
Highlights
Gold nanoparticles (AuNPs) have amazing chemical–physical features that make them appealing for biotechnology and medical applications [1,2,3,4,5]
There are many issues that need to be addressed, such as the biological interaction of the nanocarrier in patients, the knowledge of the molecular mechanisms that drive nanoparticle-cell interactions, the barriers to marketing related to manufacturing, costs and regulatory standards, today research is investing heavily in this area, seeking to minimize the complexity of nanomaterials by taking into account the final form and dosage for human use, so that a formulation has the potential to be translated into clinically applicable therapies [13,14]
The surface functionalization of gold nanoparticles is crucial for the effective utilization of these materials in health-related applications and hydrophilic molecules, such as thiols, amines or polymers, can provide a suitable way to introduce reactive functional groups that can be utilized for targeting and conjugating therapeutic agents [22,23,24,25]
Summary
Gold nanoparticles (AuNPs) have amazing chemical–physical features that make them appealing for biotechnology and medical applications [1,2,3,4,5]. Very few scientific publications (i.e., less than 20 present in the pubmed site) addressed the efficacy of gold-conjugated RSV nanoparticles as a therapeutic agent Most of these papers focused on the ability of RSV to maintain its antibacterial activity [43], antioxidant properties [44,45], anti-hepatoma [46], anti-breast cancer cell invasion [47], and anti-diabetic [48] effects. AuNPs functionalized with hydrophilic capping agents, i.e., sodium citrate (cit) and L-Cysteine (L-cys), were synthesized and deeply investigated These AuNPs were used to conjugate RSV, improving its bioavailability. The biocompatibility of AuNPs and AuNPs@RSV1 was evaluated in a concentration range of 1.0–45.5 μg/mL by assessing their effects on breast cancer cell, MCF-7, viability
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