Anti-EGFR-Coated Gold Nanoparticles In Vitro Carry 5-Fluorouracil to Colorectal Cancer Cells

Abstract

The aim of the current study is to present a strategy to improve the efficiency of 5-fluorouracil (5-FU), which is widely used as antineoplastic agent against solid tumors-based on the use of gold nanocarriers to overcome the resistance of colorectal cancer cells. 5-FU was loaded on gold nanoparticles (AuNP) coated with anti-EGFR antibodies in order to target them towards colorectal cancer cells that overexpress epidermal growth factor receptors (EGFR). Physicochemical characterization has shown that AuNP size was approximately 20 nm and that AuNP functionalization led to spherical nanoparticles. Flow cytometry allowed observing that some compounds synthesized by our research group have induced apoptosis/necrosis and impaired the proliferation of colon cancer cell lines ‘HCT-116′ and ‘HT-29′. The antibody/drug combination in AuNP (AuNP 5FU EGFR) has improved the apoptosis rate and impaired cell proliferation in both cell lines, regardless of the exposure time. Overall, these results have shown that AuNP functionalization with monoclonal antibodies focused on delivering 5-FU to tumor cells is an exciting strategy against colorectal cancer.

Evaluating the Targeting Efficiency of Anti-EGFR Functionalised Nanoparticles to Head and Neck Cancer Cells for Use in NIR-II Optical Window

“…This in vitro study identified that anti-EGFR functionalisation increased the targeting potential of the AuNRs to EGFR expressing cell lines. Our findings in this study are supported by other studies including colorectal cancer [26], cervical cancer [27], skin cancer [28] and others where each of them found an increased uptake of functionalised gold nanoparticles in EGFR expressing cancer cells. In our study, although we used two cancer cell lines with an almost equal level of EGFR expression as shown by flow cytometry (Fig.…”

“…All four cancer cell lines were cultured in triplicate, on a 22 mm x 22 mm glass coverslips, as described previously. Biotinylated anti-EGFR monoclonal antibody was conjugated with AuNRs as described above [25] [24][25][26]. After culturing the cells for 24 hr on coverslips, the supernatants were removed and either tAuNRs or uAuNRs in 2 ml fresh complete medium were added into each well.…”

Biocompatible DNA/5-Fluorouracil-Gemini Surfactant-Functionalized Gold Nanoparticles as Promising Vectors in Lung Cancer Therapy

“…Its serious side effects, including severe gastrointestinal toxicity, hematologic disturbance, and heart toxicosis, limit its clinical benefits [ 38 ]. In this sense, a new strategy for improving 5-Fu efficiency was developed by Liszbinski and coworkers based on 5-Fu loading on gold nanoparticles coated with epidermal growth factor receptors antibodies (anti-EGFR) for colorectal cancer treatment [ 39 ]. Other recent approaches for improving the colon delivery of 5-fluoracyl include the preparation and optimization of 5-Fu-loaded biogenic gold nanoparticles with pluronic-based coatings [ 40 ].…”

Current Landscape in Organic Nanosized Materials Advances for Improved Management of Colorectal Cancer Patients

“…Antibodies are also widely used for nanocarrier functionalization based on their inherent capability to specifically recognize their targets, and the promising results of cetuximab and panitumumab administration in improving clinical outcomes for mCRC patients lead to the use of these molecules as functionalization agents to direct nanoparticles towards tumor cells that overexpress EGFR. Several anti-EGFR-coated nanoparticles loaded with 5-FU were synthesized for CRC applications and showed superior colorectal cancer cell specificity and cytotoxicity of the novel drug-delivery systems [ 123 , 124 , 125 ]. An alternative for antibody use are aptamers, small single-stranded DNA or RNA molecules that present superior binding specificity and affinity for targeted molecules and low immunogenicity [ 126 ].…”