Functionalized gold nanoparticles improve afatinib delivery into cancer cells

• Type: Article in International Scientific Journal
• Date: 2016

Authors

Sílvia Castro Coelho (Author) FEUP; Gabriela M. Almeida (Author) Other; Maria do Carmo Pereira (Author) FEUP; Filipe Santos-Silva (Author) Other; Manuel A. N. Coelho (Author) FEUP

Journal

Title: Expert Opinion on Drug Delivery

Vol. 13 No. 1

Pages: 133-141

ISSN: 1742-5247

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 16 Citations

Scopus - 23 Citations

Scientific classification

FOS: Engineering and technology > Nano-technology

Associated Projects

NanoEFEct - Nanoparticle enhanced molecular Fluorescence-Endoscopy for detection of early stage colorectal adenocarcinoma

Other information

Authenticus ID: P-00J-Z3Q

DOI: 10.1517/17425247.2015.1083973

Abstract (EN): Objectives: A drug delivery system based on colloidal pegylated gold nanoparticles (PEGAuNPs) conjugated with the tyrosine kinase inhibitor afatinib was designed and tested for enhancing the drug activity against pancreatic and NSCLC cells. Methods: PEGAuNPs were synthesized and characterized physicochemically. Confocal imaging was performed to evaluate the nanoparticle (NP) internalization in cancer cells. For cell-cycle distribution analysis, conjugated NPs and afatinib alone were incubated with cells and alterations on the cell-cycle profile subsequently analyzed by total DNA staining. Cancer cell survival and growth inhibition following incubation with afatinib and PEGAuNPs-afatinib (concentrations between 0.007 and 0.500 mu M afatinib) were evaluated. Results: A higher cellular uptake of PEGAuNPs was observed by cancer cells. Our data suggest an efficient conjugation of PEGAuNPs with the drug, enhancing the afatinib activity in comparison with afatinib alone. In fact, IC50 and GI(50) results obtained show that the PEGAuNPs-afatinib conjugate is ca. 5 and 20 times more potent than afatinib alone in S2-013 and A549 cell lines, respectively. Conclusions: Conjugating PEGAuNPs with afatinib is a promising antitumor delivery system for cancer therapy as it improves drug efficacy, allowing a reduction in drug dose used and minimizing possible toxicity-related side effects.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9