Influence of PEG coating on the oral bioavailability of gold nanoparticles in rats

Abstract

Metallic nanoparticles can be produced in a variety of shapes, sizes, and surface chemistries, making them promising potential tools for drug delivery. Most studies to date have evaluated uptake of metallic nanoparticles from the GI tract with methods that are at best semiquantitative. This study used the classical method of comparing blood concentration area under the curve (AUC) following intravenous and oral doses to determine the oral bioavailability of 1, 2 and 5 kDa PEG-coated 5 nm gold nanoparticles (AuNPs). Male rats were given a single intravenous dose (0.8 mg/kg) or oral (gavage) dose (8 mg/kg) of a PEG-coated AuNP, and the concentration of gold was measured in blood over time and in tissues (liver, spleen and kidney) at sacrifice. Blood concentrations following oral administration were inversely related to PEG size, and the AUC in blood was significantly greater for the 1 kDa PEGcoated AuNPs than particles coated with 2 or 5 kDa PEG. However, bioavailabilities of all of the particles were very low (50.1%). Concentrations in liver, spleen and kidney were similar after the intravenous doses, but kidney showed the highest concentrations after an oral dose. In addition to providing information on the bioavailability of AuNPs coated with PEG in the 1-5 kDa range, this study demonstrates the utility of applying the blood AUC approach to assess the quantitative oral bioavailability of metallic nanoparticles.

Effects of major parameters of nanoparticles on their physical and chemical properties and recent application of nanodrug delivery system in targeted chemotherapy

“…The results of this in vivo study showed that both TGNPs and LTGNPs have an improved curative effect and low toxicity, and the synergistic effect produced by LTGNPs can improve the properties of the particles. 117 Alalaiwe et al conducted a test in order to evaluate the quantitative oral bioavailability of PEG-coated GNPs in rats by measuring the concentration of gold in the blood, liver, spleen, and kidneys of rats at different time intervals after oral administration of a certain dose of GNPs; 118 however, this classical approach to analyze bioavailability needs more studies. In recent years, hyperthermia and photodynamic therapy have received considerable attention, and numerous studies have shown their great potential for cancer treatment.…”

Bio-functionalized gold nanoparticles: Benign effect in Sprague-Dawley rats by intravenous administration

“…The intravenous and oral doses study shows the bioavailability of 1, 2 and 5 kDa PEG-coated 5 nm gold nanoparticles (AuNPs) in male rats. The oral dose revealed the highest concentrations of NP in kidneys and similar concentrations in different organs on intravenous doses (Alalaiwe et al, 2017). Our study revealed AuNP intravenous administration has no toxicity in the organs of rats, which supports the practice of biofunctionalized AuNP with further detail molecular study for the treatment and drug delivery in diseases.…”

Influence of chitosan coating on the oral bioavailability of gold nanoparticles in rats

“…Gold nanoparticles of approximately 3 nm were fabricated by the method reported elsewhere (Alalaiwe et al, 2017). The nanoparticles, which formed rapidly upon addition of the sodium borohydride, were then allowed to stand overnight prior to coating.…”

“…We have previously investigated the oral bioavailability of gold nanoparticles in rats, wherein, gold nanoparticles of approximately 5 nm were coated with 1, 2 and 5 kDa of polyethylene glycol (PEG) (Alalaiwe et al, 2017). PEG coating was supposed to enhance the oral bioavailability of the nanoparticles as it known to minimize the immune system recognition and elimination, thereby increasing circulatory half-life (Alalaiwe et al, 2017). Furthermore, PEG coating has also been reported to minimize the agglomeration of nanoparticles (Hinkley et al, 2015).…”