Synthesis of Diagnostic Silicon Nanoparticles for Targeted Delivery of Thiourea to Epidermal Growth Factor Receptor-Expressing Cancer Cells

Abstract

ABSTRACT:The novel thiourea-functionalized silicon nanoparticles (SiNPs) have been successfully synthesized using allylamine and sulforaphane, an important anticancer drug, followed by a hydrosilylation reaction on the surface of hydrogen terminated SiNPs. Their physiochemical properties have been investigated by photoluminescence emission, FTIR and elemental analysis. MTT assay has been employed to evaluate in vitro toxicity in colorectal cancer cells (Caco-2) and primary normal cells (CCD). The results show significant toxicity of thiourea SiNPs after 72 h incubation in the cancer cell line and the toxicity is concentration dependent and saturated for concentrations above 100 µg/mL. Confocal microscopy images have demonstrated the internalization of thiourea-functionalized SiNPs inside the cells. Flow cytometry data has confirmed receptor-mediated targeting in cancer cells. This nanocomposite takes advantage of the EGFR active targeting of the ligand in addition to the photoluminescence properties of SiNPs for bioimaging purposes. The results suggest that this novel nanosystem can be extrapolated for active targeting of the receptors that are overexpressed in cancer cells such as EGFR using the targeting characteristics of thiourea-functionalized SiNPs and therefore encourage further investigation and development of anticancer agents specifically exploiting the EGFR inhibitory activity of such nanoparticles.

Synthesis and characterisation of isothiocyanate functionalised silicon nanoparticles and their uptake in cultured colonic cells

“…24 As detailed in supporting information Figure S2 and S3, it was observed that for ITC SiNPs, at an excitation wavelength of 360 nm, the photoluminescence quantum yield (PLQY) was measured to be about 13%, which complies with previous investigations that cite values of up to 25% PLQY. [25][26][27]…”

Synthesis, crystal structure, computational analysis and biological properties of 1-(4-chlorobenzoyl)-3-[2-(2-{2-[3-(4-chlorobenzoyl)-thioureido]-ethoxy}ethoxy)ethyl]-thiourea and its Ni(II) and Cu(II) complexes

“…The hydrogen bonding ability of thiourea moieties has been utilized in the construction of anion receptors [13,14]. The high binding and ion receptive ability of thioureas are properties being exploited in their use as chemotherapeutics [15,16]. Higher hydrogen bonding interaction has been associated with increased target specificity to nuclear bases of DNA and oxidative cleavage of DNA, thereby enhancing anticancer activity [17].…”

Drug Delivery with Porous Silicon

“…The latter is relatively rarely studied applications, but promising results considering, e.g., chronotherapeutic applications have been reported (Leong et al 2007). In addition, the combination of imaging (or monitoring) and therapy in the same system (theranostics) has attracted researchers lately (Wang et al 2015a, b;Behray et al 2016;Tong et al 2016;Joo et al 2015;Hou et al 2015;Barnes and Prestidge 2015) and will surely gain more interest in the future, because PSi has many advantages for these types of applications.…”